BORON CONTAINING COMPOUNDS AND THEIR USES Cross-Reference to Related Applications [0001] The present application claims the benefit of and priority to United States Provisional Application Serial No.63/148,758, filed 12 February 2021, and United States Provisional Application Serial No.63/063,766, filed 10 August 2020, each of which is herein incorporated by reference in its entirety. Technical Field [0002] The present disclosure contemplates novel boron-containing compounds and their uses as active agents that exhibit pesticidal activity such as antimicrobial, insecticidal, arachnicidal, and/or antiparasitic activity. An agrochemical composition containing such a compound and its use in, animal health, agriculture, or horticulture is also contemplated. A method for promoting plant performance and/or reducing, ameliorating, or controlling microbes, insects, arachnids, and/or parasites on or in an animal, a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables is also contemplated. Background Art [0003] Within the field of plant health, pests such as microbes, insects, arachnids, and parasites lead to a wide range of diseases across all crops, resulting in massive losses (e.g., rusts, spots, downy mildews, blasts, blotches, stripes, rots, smuts, wilt, root knot nematode disease, fire blight, insects, etc.). Solutions are limited; currently available, conventional, and outdated chemical pesticides provide only a partial level of control (as with resistant cultivars), or add significant cost. Whereas breeding for resistance traits to specific crop/pathogen combinations in germplasm offers some hope in circumventing these problems, it is widely recognized that novel pesticidal compounds such as antimicrobial, insecticidal, arachnicidal, and/or antiparasitic compounds must be discovered. [0004] Current pesticidal compounds are typically costly to both purchase and use, and are often toxic and may be otherwise detrimental to off-target animals and/or vegetation near the site of application including runoff and affecting the watershed. Moreover, many such compounds lose efficacy over time, in part due to the rise of pests becoming resistant to treatment. Nonetheless, agrochemical pesticidal compounds such as antimicrobial, insecticidal, arachnicidal, and/or antiparasitic compounds are important to control various diseases and minimize crop loss. [0005] Parasitic infections in animals, including humans, are responsible for significant suffering and economic loss globally. Endoparasitic infections and in particular helminthiases caused by nematodes (such as roundworms including filarial worms) and flatworms [such as cestodes (tapeworms) and trematodes (flukes)], are exemplary of such parasitic infections. Such worm- born infections may inflict significant disease and damage to various organ systems. Illustratively, the gastrointestinal tract, the lymphatic system, various tissues, the liver, lungs, heart, and the brain may be damaged with sequelae that include neurological and metabolic dysfunction, nutritional deficiencies, delayed growth, loss of productivity, and death. [0006] Accordingly, there is a need for additional antimicrobial, insecticidal, arachnicidal, antifungal, and/or antiparasitic compounds and compositions for plant and animal health. [0007] Boron is an element that may be used in addition to the more traditional elements, carbon, hydrogen, oxygen, nitrogen, and phosphorous, to create powerful biologically effective compounds. Although the use of naturally occurring borates is well known, the construction and characterization of more complex, rationally designed boron-containing synthetic compounds exhibiting low toxicity and biological efficacy have been relatively under-investigated. [0008] Additionally, the boron atom’s empty p-orbital readily forms reversible covalent bonds with Lewis bases, which may affect biological activity. These characteristics together make the development of compounds that display desired biological activity an unpredictable and challenging endeavor. [0009] The creation and commercialization of boron-containing molecules has traditionally been stymied due to these synthetic and pharmacological uncertainties. [0010] An exemplary group of boron-containing biologically active compounds is referred to in the literature as 1,2-dihydro-1-hydroxy-2,3,1-benzodiazaborines [Gu et al., Org Biomol Chem 15:7543-7548 (2017) and Kanichar et al., Chem Biodivers, 11:1381-1397 (2014)]. A hypothetical structural formula for a substituted 1,2-dihydro-1-hydroxy-2,3,1-benzodiazaborine is illustrated in Formula A, below, wherein numbered substituent positional locations are noted within the rings. [0011] Substituents bonded to the 2-position N-acyl group carbon atom (R ² ) and the 4-position ring carbon atom (R ¹ ) are undefined for convenience. The above ring positional nomenclature system may be used throughout the disclosure. [0012] In some emboidments, a contemplated substituted 1,2-dihydro-1-hydroxy-2,3,1- benzodiazaborine (an acyl diazaborine) may exist in one or more of three structural forms that are referred to herein as, closed (ex I), anhydrodimer (ex II), and open or hydrazone (ex III). The open, hydrazone form may also exist as two stereoconformational isomers. The three forms (closed, anhydrodimer, and open) are illustrated in Illustrative Example 1, below, for a hypothetical compound. Illustrative Example 1 [0013] Each of the above possible structures (ex I), (ex II), and (ex III), of a substituted acyl benzodiazaborine theoretically may form. Illustratively, the closed form of the product may be formed and exist in an organic solvent possessing a small amount of water. See Gu et al., Org Biomol Chem, 15:7543-7548 (2017). [0014] The present invention helps to fill the above-discussed pesticidal (particularly antimicrobial and more particularly antifungal) needs with new compounds, compositions containing them, and methods of using them, as well as the use of older compounds in new pesticidal (particularly antimicrobial) methods of treatment. Brief Summary of The Invention [0015] It has been found that a particular group of boron-containing compounds exhibit pesticidal (particularly antimicrobial) activity such as one or more selected from the group consisting of: antimicrobial, insecticidal, arachnicidal, and antiparasitic. This contemplated compound group of compounds may be referred to as substituted 1,2-dihydro-1-hydroxy-2,3,1- benzodiazaborines. In a preferred embodiment of the present disclosure, the boron-containing compounds exhibit antifungal activity. [0016] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas I, II and III:

or a salt thereof, wherein for each Y is O or S, where, for Formula II, each Y is the same; X is halogen, CN, S(C ₁ -C ₃ hydrocarbyl), or O(C ₁ -C ₃ hydrocarbyl); n is a number selected from the group consisting of zero, 1, 2, 3, and 4, such that when n is zero, X is absent; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and R ² is selected from the group consisting of: substituted or unsubstituted C ₁ -C ₆ hydrocarbyl, substituted or unsubstituted C ₃ -C ₆ cyclohydrocarbyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein said substituted aryl group is a substituted phenyl or substituted naphthyl group that when substituted contains one, two, or three substituents independently selected from the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl); wherein an said heteroaryl group contains 1 ring or 2 fused aromatic rings that include 1, 2, or 3 ring heteroatoms that are the same or different, and are nitrogen, oxygen, or sulfur; and when substituted, said heteroaryl group is substituted with one, two, or three substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , O(C ₁ -C ₆ hydrocarbyl), O( C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, C ₃ -C ₆ cyclohydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), NHSO ₂ ( C ₃ -C ₆ cyclohydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ (C ₃ -C ₆ cyclohydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl). [0017] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas I, II and III: or a salt thereof, wherein for each Y is O or S, where, for Formula II, each Y is the same; X is halogen, CN, S(C ₁ -C ₃ hydrocarbyl), O(C ₁ -C ₃ hydrocarbyl), aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is a number selected from the group consisting of zero, 1, 2, 3, and 4, such that when n is zero, X is absent; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and R ² is selected from the group consisting of: substituted or unsubstituted C ₁ -C ₆ hydrocarbyl, substituted or unsubstituted C ₃ -C ₆ cyclohydrocarbyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein in each instance a substituted aryl group is a substituted phenyl or substituted naphthyl group that when substituted contains one, two, or three substituents independently selected from the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl); wherein an said heteroaryl group contains 1 ring or 2 fused aromatic rings that include 1, 2, or 3 ring heteroatoms that are the same or different, and are nitrogen, oxygen, or sulfur; and when substituted, said heteroaryl group is substituted with one, two, or three substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, C ₃ -C ₆ cyclohydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), NHSO ₂ (C ₃ -C ₆ cyclohydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ (C ₃ -C ₆ cyclohydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl). [0016] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas Ia, IIa, and IIIa: or a salt form thereof, wherein: Y is O or S, where, for Formula IIa, each Y is the same; X is halogen, CN, S(C ₁ -C ₃ hydrocarbyl), or O(C ₁ -C ₃ hydrocarbyl); n is a number selected from the group consisting of: zero, 1, 2, 3, and 4, such that when n is zero, X is absent; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and when n is 1 or more, R ² is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, substituted C ₃ – C ₆ cyclohydrocarbyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, substituted heteroaryl, wherein the substitued C ₁ – C ₆ hydrocarbyl, substitued C ₃ – C ₆ cyclohydrocarbyl, substituted phenyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C3 – C6 cyclohydrocarbyl; and when n is zero, R ² is R ^2a , wherein: R ^2a is C1 – C6 hydrocarbyl, substituted C1 – C6 hydrocarbyl, C3 – C6 cyclohydrocarbyl, substituted C3 – C6 cyclohydrocarbyl, naphthyl, substituted naphthyl, unsubstituted heteroaryl other than pyridyl, or substituted heteroaryl, wherein the substituted C1 – C6 hydrocarbyl, substituted C3 – C6 cyclohydrocarbyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C3 – C6 cyclohydrocarbyl; or R ^2a is substituted phenyl that has 2 or 3 substituents selected from the group consisting of: OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially and fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially and fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₁ -C ₃ hydrocarbyl), or R ^2a is substituted phenyl that has 1 substituent selected from the group consisting of: OH, O(C1- C6 hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C1- C6 partially or fully halogenated hydrocarbyl), partially or fully halogenated C ₁ -C ₆ hydrocarbyl, SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), halogen that is meta to the point of attachment to the remainder of the molecule, C ₁ -C ₆ hydrocarbyl that is ortho or meta to the point of attachment to the reminder of the molecule; wherein, for a compound of structural formula Ia, one X may combine with the depicted oxygen bonded to the boron atom to form a 5 to 8 membered ring, which may contain one or more additional heteroatoms selected from N, O, and S; wherein each of said phenyl or substituted phenyl groups may be attached through a divalent C ₁ – C ₃ hydrocarbyl group; and wherein each heteroaryl group contains 1 ring or 2 fused rings that include 1, 2, or 3 ring heteroatoms that are the same or different and are selected from one or more of nitrogen, oxygen, and sulfur. [0017] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas Ia, IIa, and IIIa:

or a salt form thereof, wherein: Y is O or S, where, for Formula IIa, each Y is the same; X is halogen, CN, S(C ₁ -C ₃ hydrocarbyl), O(C ₁ -C ₃ hydrocarbyl), aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is a number selected from the group consisting of: zero, 1, 2, 3, and 4, such that when n is zero, X is absent; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and when n is 1 or more, R ² is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ -C ₆ cyclohydrocarbyl, substituted C ₃ -C ₆ cyclohydrocarbyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, substituted heteroaryl, wherein the substitued C ₁ – C ₆ hydrocarbyl, substitued C ₃ -C ₆ cyclohydrocarbyl, substituted phenyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C ₃ – C ₆ cyclohydrocarbyl; and when n is zero, R ² is R ^2a , wherein: R ^2a is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, substituted C ₃ – C ₆ cyclohydrocarbyl, naphthyl, substituted naphthyl, unsubstituted heteroaryl other than pyridyl, or substituted heteroaryl, wherein the substituted C ₁ – C ₆ hydrocarbyl, substituted C ₃ – C ₆ cyclohydrocarbyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C ₃ – C ₆ cyclohydrocarbyl; or R ^2a is substituted phenyl tat has 2 or 3 substituents selected from the group consisting of: OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially and fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially and fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₁ -C ₃ hydrocarbyl), or R ^2a is substituted phenyl that has 1 substituent selected from the group consisting of: OH, O(C ₁ - C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ - C ₆ partially or fully halogenated hydrocarbyl), partially or fully halogenated C ₁ -C ₆ hydrocarbyl, SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), halogen that is meta to the point of attachment to the remainder of the molecule, C ₁ -C ₆ hydrocarbyl that is ortho or meta to the point of attachment to the reminder of the molecule; wherein, for a compound of structural formula Ia, one X may combine with the depicted oxygen bonded to the boron atom to form a 5 to 8 membered ring, which may contain one or more additional heteroatoms selected from N, O, and S; wherein each of said phenyl or substituted phenyl groups may be attached through a divalent C ₁ – C ₃ hydrocarbyl group; and wherein each heteroaryl group contains 1 ring or 2 fused rings that include 1, 2, or 3 ring heteroatoms that are the same or different and are selected from one or more of nitrogen, oxygen, and sulfur. [0018] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas I, II and III: or a salt thereof, wherein for each Y is O or S, where, for Formula IIa, each Y is the same; X is aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is a number selected from the group consisting of: 1, 2, 3, and 4; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and R ² is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, substituted C ₃ – C ₆ cyclohydrocarbyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, substituted heteroaryl, wherein the substitued C ₁ – C ₆ hydrocarbyl, substitued C ₃ – C ₆ cyclohydrocarbyl, substituted phenyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C ₃ – C ₆ cyclohydrocarbyl. [0019] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas Ia, IIa, and IIIa: or a salt form thereof, wherein: Y is O or S, where, for Formula IIa, each Y is the same; X is halogen, CN, S(C ₁ -C ₃ hydrocarbyl), O(C ₁ -C ₃ hydrocarbyl), aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is a number selected from the group consisting of: zero, 1, 2, 3, and 4, such that when n is zero, X is absent; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and when n is 1 or more, R ² is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, substituted C ₃ – C ₆ cyclohydrocarbyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, substituted heteroaryl, wherein the substitued C ₁ – C ₆ hydrocarbyl, substitued C3 – C6 cyclohydrocarbyl, substituted phenyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C3 – C6 cyclohydrocarbyl; and when n is zero, R ² is R ^2a , wherein: R ^2a is C1 – C6 hydrocarbyl, substituted C1 – C6 hydrocarbyl, C3 – C6 cyclohydrocarbyl, substituted C3 – C6 cyclohydrocarbyl, naphthyl, substituted naphthyl, unsubstituted heteroaryl other than pyridyl, or substituted heteroaryl, wherein the substituted C1 – C6 hydrocarbyl, substituted C3 – C6 cyclohydrocarbyl, substituted naphthyl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C3 – C6 cyclohydrocarbyl; or R ^2a is substituted phenyl that has 2 or 3 substituents selected from the group consisting of: OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially and fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially and fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₁ -C ₃ hydrocarbyl), or R ^2a is substituted phenyl that has 1 substituent selected from the group consisting of: OH, O(C ₁ - C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ - C ₆ partially or fully halogenated hydrocarbyl), partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), halogen that is meta to the point of attachment to the remainder of the molecule, C ₁ -C ₆ hydrocarbyl that is ortho or meta to the point of attachment to the reminder of the molecule; wherein, for a compound of structural formula Ia, one X may combine with the depicted oxygen bonded to the boron atom to form a 5 to 8 membered ring, which may contain one or more additional heteroatoms selected from N, O, and S; wherein each of said phenyl or substituted phenyl groups may be attached through a divalent C ₁ – C3 hydrocarbyl group; and wherein each heteroaryl group contains 1 ring or 2 fused rings that include 1, 2, or 3 ring heteroatoms that are the same or different and are selected from one or more of nitrogen, oxygen, and sulfur. [0020] In one aspect, R ¹ is hydrogen. In one aspect, Y is O. [0021] In one aspect, n is 1. In one aspect, X is halogen. In one aspect, X is chlorine. [0022] In one aspect, the compound is of one, two, or all of structural Formulas Ib, IIb, and IIIb: [0023] In one aspect, R ² is phenyl or substituted phenyl. [0024] In one aspect, R ² is phenyl substituted with one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C ₃ – C ₆ cyclohydrocarbyl. [0025] In one aspect, R ² is phenyl substituted with one or more of the group consisting of: O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, and partially or fully halogenated C ₁ -C ₆ hydrocarbyl. [0026] In one aspect, R ² is phenyl substituted with one or more of the group consisting of: O(C ₁ -C ₃ hydrocarbyl), O(C ₁ -C ₃ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₃ hydrocarbyl), S(C ₁ -C ₃ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₃ hydrocarbyl, and partially or fully halogenated C ₁ -C ₃ hydrocarbyl. [0027] In one aspect, R ² is phenyl or phenyl substituted with halogen. [0028] In one aspect, R ² is phenyl or substituted phenyl and is attached through a divalent C1 – C3 hydrocarbyl group. [0029] In one aspect, R ² is substituted with one substituent. [0030] In one aspect, R ² is a substituted phenyl, substituted naphthyl, or substituted heteroaryl group. [0031] In one aspect, R ² is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, or substituted C ₃ – C ₆ cyclohydrocarbyl. [0032] In one aspect, R ² is heteroaryl or substituted heteroaryl. In one aspect, the heteroaryl group that is substituted or unsubstituted is selected from the group consisting of: pyridine, thiophene, thiazole, imidazole, benzimidazole, pyrazole, and oxazole. In one aspect, the heteroaryl group that is substituted or unsubstituted is selected from the group consisting of: thiophene, thiazole, imidazole, benzimidazole, pyrazole, and oxazole. [0033] In one aspect, R ² is substituted with one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C ₃ – C ₆ cyclohydrocarbyl. [0034] In one aspect, R ² is heteroaryl substituted with one or more of the group consisting of O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, and partially or fully halogenated C ₁ -C ₆ hydrocarbyl. [0035] In one aspect, the halogen of said partially or fully halogenated hydrocarbyl is fluorine or chlorine. [0036] In one aspect, n is 0. [0037] In one aspect, R ^2a is is selected from the group consisting of: substituted phenyl, susbtitued naphthyl, benzyl, heteroaryl, and substituted heteroaryl. [0038] In one aspect, R ^2a is a substituted phenyl, substituted naphthyl, heteroaryl, or substituted heteroaryl. In one aspect, the heteroaryl group that is substituted or unsubstituted is selected from the group consisting of: pyridine, thiophene, thiazole, imidazole, benzimidazole, pyrazole, and oxazole. In one aspect, the heteroaryl group that is substituted or unsubstituted is selected from the group consisting of: thiophene, thiazole, imidazole, benzimidazole, pyrazole, and oxazole. In one aspect, the heteroaryl group contains two ring heteroatoms. [0039] In one aspect, R ^2a is substituted with one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C3 – C6 cyclohydrocarbyl. [0040] In one aspect, the R ^2a substituent contains a halogen. In one aspect, halogen is fluorine or chlorine. [0041] In one aspect, R ^2a is selected from phenyl substituted with O(C ₁ -C ₆ hydrocarbyl), phenyl substituted with halogen, phenyl substituted with S(C ₁ -C ₆ hydrocarbyl) and heteroaryl substituted with halogen. [0042] In one embodiment, the compound corresponds to Formula Ia. In one embodiment, the compound corresponds to Formula IIa. In one embodiment, the compound corresponds to Formula IIIa. [0043] One embodiment of the present disclosure includes a compound or a salt thereof selected from the group consisting of Compound List A: Compound List A

[0045] In one aspect, the compound is in a corresponding open form. In one aspect, the compound is in a corresponding anhydrodimer form thereof. [0046] One embodiment of the present invention includes a compound or a salt thereof selected from the group consisting of Compound List B: Compound List B: Compound List B

[0047] In one aspect, the compound is in a corresponding open form thereof. In one aspect, the compound is in a corresponding anhydrodimer form thereof. [0048] One embodiment of the present disclosure includes a compound or a salt thereof selected from the group consisting of Compound List C: Compound List C:

[0049] In one aspect, the compound is in a corresponding open form thereof. In one aspect, the compound is in a corresponding anhydrodimer form thereof. [0050] One embodiment of the present disclosure includes a compound or a salt thereof selected from the group consisting of Compound List D: Compound List D [0051] One embodiment of the present disclosure includes a compound or a salt thereof selected from the group consisting of Compound List E: Compound List E _[ 0052] In one aspect, the compound is substantially free of a corresponding closed or monomer form thereof. In one aspect, the compound is substantially free of a corresponding anhydrodimer form thereof. [0053] One embodiment of the present disclosure includes a compound that is of structural formula Ia and one X combines with the depicted oxygen and boron atoms to form a 5 to 8 membered ring, which may contain one or more additional heteroatoms selected from N, O, and S. In one aspect, the one or more additional heteroatoms is one O. In one aspect, the compound is wherein each of X, Y, and R ² is as defined. [0054] One embodiment of the present disclosure includes a compound of one, two, or all of structural Formulas Ic, IIc, and IIIc: , or a salt thereof, wherein for each Y is O or S, where, for Formula IIa, each Y is the same; X is unsubstituted aryl, substituted aryl, unsubstituted heteroaryl, or substituted heteroaryl; n is a number selected from the group consisting of: 1, 2, 3, and 4; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and R ² is C ₁ – C ₆ hydrocarbyl, substituted C ₁ – C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, substituted C ₃ – C ₆ cyclohydrocarbyl, unsubstituted aryl, substituted aryl, unsubstituted heteroaryl, or substituted heteroaryl, wherein the substitued C ₁ – C ₆ hydrocarbyl, substitued C ₃ – C ₆ cyclohydrocarbyl, substituted aryl, or substituted heteroaryl group has 1, 2, or 3 substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and C3 – C6 cyclohydrocarbyl. [0055] In one aspect, n is 1. In one aspect, X is aryl or substituted aryl. In one aspect, X is unsubstitued naphthyl, substituted naphthyl, substituted phenyl, or unsubstituted phenyl. In one aspect, X is substituted phenyl or unsubstituted phenyl. In one aspect, X is substituted phenyl, and has one or more substiuent selected from the group consisting of halogen, O(C ₁ -C ₃ hydrocarbyl), and S(C ₁ -C ₃ hydrocarbyl). In one aspect, X is substituted or unsubstituted heteroaryl, wherein heteroayl is a 5- to 9- membered single ring or two fused ring group containing from one to four heteroatoms selected from nitrogen, oxygen, and sulfur, where the nitrogen and sulfur atoms are optionally oxidized, and one or several nitrogen atoms are optionally quaternized. In one aspect, heteroaryl is indazole. In one aspect, the heteroaryl group is attached to the remainder of the molecule through a heteroatom. [0056] In one aspect, R ² is unsubstituted C ₁ -C ₆ hydrocarbyl, substituted C ₁ -C ₆ hydrocarbyl, unsubstituted phenyl, substituted phenyl, substituted heteroaryl, or unsubstituted heteroaryl. In one aspect, R ² is unsubstituted phenyl substituted phenyl, unsubstituted heteroaryl, or substituted heteroaryl wherein the substituted phenyl or substituted heteroaryl are have a substituent selected from the group consisting of: halogen and C1 – C6 hydrocarbyl. In one aspect, wherein R ² is substituted or unsubstituted phenyl. In one aspect, a substituted phenyl has one or more substituent selected from the group consisting of fluorine and chlorine. In one aspect, R ² is substituted heteroaryl or unsubstituted heteroaryl, wherein heteroayl is a 5- to 9- membered single ring or two fused ring group containing from one to four heteroatoms selected from nitrogen, oxygen, and sulfur, where the nitrogen and sulfur atoms are optionally oxidized, and one or several nitrogen atoms are optionally quaternized. In one aspect, the heteroaryl group is attached to the remainder of the molecule through a heteroatom. In one aspect, the substituted or unsubstituted heteroaryl is thiazole. In one aspect, each of X and R ² independently is unsubstituted phenyl or phenyl substituted with a halogen. [0057] In one aspect, the compound is of one, two, or all of structural Formulas Ic, IIc, and IIIc: R ¹ X ). [0058] In one aspect, R ¹ is hydrogen. In one aspect, Y is O. [0059] In one aspect, the compound corresponds to Formula I. In one aspect, the compound corresponds to Formula II. In one aspect, the compound corresponds to Formula III. [0060] One embodiment of the present disclosure includes a compound or a salt thereof selected from the group consisting of Compound List F: Compound List F:

[0061] In one aspect, the compound is in a corresponding open form thereof. In one aspect, the compound is in a corresponding anhydrodimer form thereof. [0062] One embodiment of the present disclosure includes a compound or salt thereof selected from the group consisting of Compound List G: Compound List G OH O B

[0063] In one aspect, the compound is in a corresponding open form thereof. In one aspect, the compound is in a corresponding anhydrodimer form thereof. [0064] One embodiment of the present disclosure includes a compound or salt thereof selected from the group consisting of: OH O B , , , ,

nd [ 0065] In one aspect, the compound is in a corresponding open form thereof. In one aspect, the compound is in a corresponding anhydrodimer form thereof. [0066] One embodiment of the present disclosure includes a method of reducing, ameliorating, or controlling an infestation of a plant or animal by a pest that comprises administering a composition comprising a pesticidal effective amount of a compound of one, two or all of structural Formulas I, II and III, below, which may be dissolved or dispersed in a carrier medium, to a plant or animal in need thereof:

wherein for each of Formulas I, II, and III: Y is O or S, where, for Formula IIb, each Y is the same; X is halogen, CN, S(C ₁ -C ₃ hydrocarbyl), O(C ₁ -C ₃ hydrocarbyl), unsubstituted aryl, substituted aryl, unsubstituted heteroaryl, or substituted heteroaryl; n is a number selected from the group consisting of zero, 1, 2, 3, and 4, such that when n is zero, X is absent; R ¹ is selected from the group consisting of: hydrogen, C ₁ -C ₄ hydrocarbyl, and C ₃ -C ₄ cyclohydrocarbyl; and R ² is selected from the group consisting of: substituted or unsubstituted C ₁ -C ₆ hydrocarbyl, substituted or unsubstituted C ₃ -C ₆ cyclohydrocarbyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein said substituted aryl group in any instance is a substituted phenyl or substituted naphthyl group that when substituted contains one, two, or three substituents independently selected from the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , OH, O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, C ₃ – C ₆ cyclohydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl); wherein said heteroaryl group in any instance contains 1 ring or 2 fused aromatic rings that include 1, 2, or 3 ring heteroatoms that are the same or different, and are nitrogen, oxygen, or sulfur; and when substituted, said heteroaryl group is substituted with one, two, or three substituents independently selected from one or more of the group consisting of: CN, (C ₁ -C ₇ ) hydrocarboyloxy, NO ₂ , O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C1- C ₆ hydrocarbyl, C ₃ -C ₆ cyclohydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), NHSO ₂ (C ₃ -C ₆ cyclohydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ (C ₃ -C ₆ cyclohydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl). [0067] In one aspect, X is unsubstitued aryl, substituted aryl, unsubstituted heteroaryl, or substituted heteroaryl. In one aspect, X is unsubstituted naphthyl, substituted naphthyl, substituted phenyl, or unsubstituted phenyl. In one aspect, X is substituted phenyl or unsubstituted phenyl. In one aspect, X is substituted phenyl, and has one or more substituent selected from the group consisting of halogen, O(C ₁ -C ₃ hydrocarbyl), and S(C ₁ -C ₃ hydrocarbyl). In one aspect, X is substituted or unsubstituted heteroaryl. In one aspect, heteroaryl is indazole. [0068] In one aspect, R ² aryl group is unsubstituted phenyl, unsubstituted naphthyl, substituted phenyl, or substituted naphthyl, wherein the substituted phenyl or substituted naphthyl has 1 or 2 substituents independently selected from the group consisting of: CN, (C1- C7) hydrocarboyloxy, NO ₂ , O(C ₁ -C ₆ hydrocarbyl), O(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), S(C ₁ -C ₆ hydrocarbyl), S(C ₁ -C ₆ partially or fully halogenated hydrocarbyl), halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, NHSO ₂ (C ₁ -C ₃ hydrocarbyl), SO ₂ NH ₂ , SO ₂ (C ₁ -C ₃ hydrocarbyl), NHC(O)(C ₁ -C ₃ hydrocarbyl), and NHC(O)(C ₃ -C ₆ cyclohydrocarbyl). [0069] In one aspect, R ² group is a substituted or unsubstituted heteroaryl group that contains 1 ring or 2 fused rings that include 1, 2, or 3 ring heteroatoms that are the same or different, and are nitrogen, oxygen, or sulfur, and said heteroaryl group’s one or two heteroaromatic rings contain a total of 5, 6, 8, 9, or 10 ring atoms. [0070] In one aspect, a substituted heteroaryl group contains at least one substituent selected from the group consisting of: halogen, C ₁ -C ₆ hydrocarbyl, partially or fully halogenated C ₁ -C ₆ hydrocarbyl, O(C ₁ -C ₆ hydrocarbyl), and partially or fully halogenated O(C ₁ -C ₆ hydrocarbyl). [0071] In one aspect, a substituted or unsubstituted heteroaryl group is selected from the group consisting of: pyridine, purine, thiophene, thiazole, imidazole, benzimidazole, pyrazole, 1,2,3- and 1,2,4-triazole, oxazole, and oxazole. [0072] One embodiment of the present disclosure includes a method of reducing, ameliorating, or controlling an infestation of a plant or animal by a pest that comprises administering a composition comprising a pesticidal effective amount of a compound of the present disclosure. [0073] One embodiment of the present disclosure includes a method of reducing, ameliorating, or controlling an infestation of a plant or animal by a pest that comprises administering a composition comprising a pesticidal effective amount of a compound selected from the group consisting of: Compound Lists C and F

[0074] In one aspect, the pest is a fungus. In one aspect, the compound is a broad spectrum fungicide. In one aspect, the fungus is soil borne. In one aspect, the fungus is of the class Plasmodiophoromycetes, Peronosporomycetes (Syn. Oomycetes), Chytridiomycetes, Zygomycetes, Ascomycetes, Basidiomycetes, or Deuteromycetes (Syn. Fungi imperfecti). [0075] In one aspect, the method is used in plant protection as foliar, seed dressing, as a soil fungicide, or combating fungi infestation in wood or roots. In one aspect, the fungus is selected from one or more members of the phyla of Ascomycota, Oomycota, Basidiomycota, and the subphylum Mucoromycotina; from the division Ascomycota, subdivision Pezizomycotina and Taphrinomycotina, Dothideomycetes, Leotiomycetes, Sordariomycetes and Taphrinomycetes classes; of the phylum Ascomycota, subphyla selected from the group consisting of Dothideomycetes, Leotiomycetes, and Sordariomycetes; fungi of the division Basidiomycota, subdivisions Agaricomycotina, Pucciniomycotina, and Ustilaginomycotina. In one aspect, the fungus is selected from one or more of the group consisting of Alternaria, Aspergillus, Bipolaris, Blumeria, Botrytis, Candida, Cercospora, Cercosporidium, Claviceps, Cochliobolus, Colletotrichum, Corynespora, Dybotryon, Dilophospora, Erysiphe, Exserohilum, Fusarium, Leveillula, Magnaporthe, Melampsora, Microsphaera, Microsphaeropsis, Monilia, Monilinia, Mycosphaerella, Oidiopsis, Peronospora, Phaeosphaeria, Phakopsora, Phomopsis, Phymatotrichum, Phytophthora, Plasmopora, Podosphaera, Pseudoperonospora, Puccinia, Pyrenophora, Pyricularia, Pythium, Rhizoctonia, Sclerophthora, Sclerotinia, Septoria, Setosphaeria, Uncinula, Ustilago, Venturia, Verticillium, and Zymoseptoria. In one aspect, the fungus is of the genus Botrytis. In one aspect, the fungus is B. cinerea. [0076] In one embodiment, the microbial infection is fungal. In one aspect, the fungal infection is a True Fungal infection or a fungal-like infection. In one aspect, the fungal infection is caused by an organism characterized as Ascomycota, Basidiomycota, Cercozoa, Chytridiomycota, Deuteromycota (fungi imperfecti), Glomeromycota, Oomycota, or Zygomycota. In one aspect, the fungal infection is caused by a fungal organism characterized as Ascomycota. In one aspect, the Ascomycota is further characterized as Pzizomycotina, Saccharomycotina, Taphrinomycotina, Arthoniomycetes, Coniocybomycetes, Dothideomycetes, Eurotiomycetes, Geoglossomycetes, Laboulbeniomycetes, Lecanoromycetes, Leotiomycetes, Lichinomycetes, Omnivoromycetes, Orbiliomycetes, Pezizomycetes, Sordariomycetes, Xylonomycetes, Lahmiales, Itchiclahmadion, Triblidiales, Saccharomycetes, Archaeorhizomyces, Neolectomycetes, Pneumocystidomycetes, Schizosaccharomycetes, or Taphrinomycetes. In one aspect, wherein the fungal infection is caused by a fungal organism characterized as Basidiomycota. In one aspect, the Basidiomycota is further characterized as Pucciniomycotina, Ustilaginomycotina, or Agaricomycotina. In one aspect, the fungal infection is caused by a fungal organism characterized as Cercozoa. In one aspect, the Cercozoa is further chracterized as Endomyxa, Phytomyxea, Plasmodiophoromycota, or Phagomyxida. In one aspect, the fungal infection is caused by a fungal organism characterized as Chytridiomycota. In one aspect, the Chytridiomycota is further characterized as Synchytriales. In one aspect, the fungal infection is caused by a fungal organism characterized as Glomeromycota. In one aspect, the Glomerocycota is further characterized as Achaeosporales, Diversisporales, Glomerales, Paraglomerales, or Nematophytales. In one aspect, the fungal infection is caused by a fungal organism characterized as Oomycota. In one aspect, the Oomycota is further characteriezed as Lagenidiales, Leptomitales, Peronosporales, Phipidiales, or Saprolegniales. In one aspect, the fungal infection is caused by a fungal organism characterized as Zygomycota. In one aspect, the Zygomycota is further characterized as Mucoromycotina, Kickxellomycotina, Entomophthoromycotina, Zoopagomycotina; Endogonales, Mucorales, Mortierellales, Asellariales, Kickxellales, Dimargaritales, Harpellales, Entomophthorales, and Zoopagales. In one aspect, the fungal infection is selected from one or more of the group consisting of Alternaria, Aspergillus, Bipolaris, Blumeria, Botrytis, Candida, Cercospora, Cercosporidium, Claviceps, Cochliobolus, Colletotrichum, Corynespora, Dybotryon, Dilophospora, Erysiphe, Exserohilum, Fusarium, Leveillula, Magnaporthe, Melampsora, Microsphaera, Microsphaeropsis, Monilia, Monilinia, Mycosphaerella, Oidiopsis, Peronospora, Phaeosphaeria, Phakopsora, Phomopsis, Phymatotrichum, Phytophthora, Plasmopora, Podosphaera, Pseudoperonospora, Puccinia, Pyrenophora, Pyricularia, Pythium, Rhizoctonia, Sclerophthora, Sclerotinia, Septoria, Setosphaeria, Stangospora, Uncinula, Ustilago, Venturia, Verticillium, and Zymoseptoria. In one aspect, the fungal infection is selected from one or more of the group consisting of Alternaria, Aspergillus, Bipolaris, Blumeria, Botrytis, Candida, Cercospora, Cercosporidium, Colletotrichum, Corynespora, Erysiphe, Fusarium, Magnaporthe, Mycosphaerella, Peronospora, Phaeosphaeria, Phakopsora, Phytophthora, Plasmopora, Podosphaera, Pseudoperonospora, Puccinia, Pyricularia, Pythium, Rhizoctonia, Sclerotinia, Septoria, Stangospora, Verticillium, and Zymoseptoria. [0077] In one embodiment, the plants or plant propagation material is agricultrual, horticultural, or ornamental. In one aspect, the plant propagation materials is seed. In one aspect, the plants or plant propagation materials are one or more of maize, soya bean, alfalfa, cotton, sunflower, Brassica oil seeds, Brassica napus, Brassica rapa, B. juncea, Brassica carinata, Arecaceae sp., Rosaceae sp., Ribesioidae sp., Juglandaceae sp., Betulaceae sp., Anacardiaceae sp., Fagaceae sp., Moraceae sp., Oleaceae sp., Actinidaceae sp., Lauraceae sp., Musaceae sp., Rubiaceae sp., Theaceae sp., Sterculiceae sp., Rutaceae sp., Solanaceae sp., Liliaceae sp., Compositae sp., Umbelliferae sp., Cucurbitaceae sp., Alliaceae sp., Cruciferae sp., Leguminosae sp., Chenopodiaceae sp., Linaceae sp., Cannabeacea sp., Malvaceae sp., Papaveraceae, Asparagaceae, Stevia rebaudiana, and genetically modifed versions thereof. In one aspect, the plants or plant propagation materials are one or more of a variety of soybean. In one aspect, the plants or plant propagation materials are one or more of the family Solanaceae sp. In one aspect, the plants or plant propagation materials are one or more of tomatoes, potatoes, peppers, tomatillo, aubergines, and tobacco. In one aspect, the plants or plant propagation materials are one or more of: (a) Fabaceae: soybean, dry beans, peanuts; (b) Poaceae: grasses including maize, wheat, rice, barley, and millet; (c) Solanaceae: tomato, potato, eggplant, peppers; (d) Cucurbitaceae: squash, pumpkin, zucchini, gourds, watermelon, melons, cucumber; (e) Rosaceae: apple, pear, quinces, apricots, plums, cherries, peaches, raspberries, strawberries, almonds; (f) Brassicaceae: broccoli, cabbage, cauliflower, kale, collards, turnips, rapeseed, radish; (g) Asteraceae or Compositae: lettuces, sunflower, artichoke; (h) Amaranthaceae: spinach, beets, chard, quinoa; (i) Convolvulaceae: sweet potato; (j) Amaryllidaceae: onion, chive, leek, garlic; (k) Ubelliferae: carrots, celery, cilantro, parsley, dill, fennel; (l) Rutaceae: citrus fruit; (m) Juglandaceae: walnut, pecan; (n) Fagaceae: oak, beeches, chesnut; (o) Pinaceae: cedar, fir, hemlock, spruce, pine; and (p) Anacardiacea: cashew, mango, pistachio. [0078] In one aspect, the compound corresponds to Formula I. In one aspect, the compound corresponds to Formula II. In one aspect, the compound corresponds to Formula III. [0079] One embodiment of the present disclosure provides a compound of the present disclosure is administered to one or more of an animal, a plant, a plant part, plant propagation material, and harvested fruits or vegetables. [0080] One embodiment of the present disclosure includes a composition comprising a compound according to the present disclosure, and one or more carrier. In one aspect, the composition is in the form of a powder. In one aspect, the composition is in the form of a liquid. In one aspect, the liquid is at least 50 percent water. In one aspect, the composition has a pH value of about 5 to about 10. [0081] One embodiment of the present disclosure includes a composition comprising a compound of the present disclosure and one or more additional active agent. In one aspect, the one or more additional active agent is selected from the group consisting of: a fungicide, a nematicide, an insecticide, and a bactericide, or any combination thereof. In one aspect, the one or more additional active agent is a fungicide. In one aspect, the fungicide has a mode as action as described by a FRAC target site code. In one aspect, the FRAC target site code is selected from the group consisting of: B1, B3, C2, C3, C4, C6, D1, E1, E2, E3, G1, H5, M4, and M5. In one aspect, the additional active agent is a fungicide selected from the group consisting of: carbendazim, thiabendazole, thiophanate, thiophanate-methyl, diethofencarb, zoxamide, ethaboxam, pencycuron, fluopicolide, metrafenone, pyriofenone, flutolanil, fluopyram, fluxapyroxad, penthiopyrad, benodanil, mepronil, isofetamid, fenfuram, carboxin, oxycarboxin, thifluzamide, benzovindiflupyr, bixafen, furametpyr, inpyrfluxam, isopyrazam, penflufen, sedaxane, isoflucypram, pydiflumetofen, pyraziflumid, boscalid, benomyl, fuberidazole, diflumetorim, tolfenpyrad, fenazaquin, azoxystrobin, coumaxystrobin, enoxastrobin, flufenoxystrobin, picoxystrobin, pyraoxystrobin, mandestrobin, pyraclostrobin, pyrametostrobin, triclopyricarb, kresoxim-methyl, trifloxystrobin, dimoxystrobin, fenamistrobin, methominostrobin, orysastrobin, famoxadone, fluoxastrobin, fenamidone, pyribencarb, cyazofamid, amisulbrom, fenpicoxamid, binapacryl, meptyldinocap, dinocap, fluazinam, ferimzone, fentin chloride, fentin acetate, fentin hydroxide, silthiofam, ametoctradin, cyprodinil, mepanipyrim, pyrimethanil, kasugamycin, blasticidin-s, quinoxyfen, proquinazid, fenpiclonil, fludioxonil, nuarimol, imazalil, oxpoconazole, pefurazoate, prochloraz, triflumizole, azaconazole, bitertanol, bromuconazole, cyproconazole, difenoconazole, diniconazole, epoxiconazole, etaconazole, fenbuconazole, fluquinconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, ipconazole, metconazole, myclobutanil, penconazole, propiconazole, simeconazole, tebuconazole, tetraconazole, triadimefon, triadimenol, triticonazole, prothioconazole, aldimorph, dodemorph, fenpropimorph, tridemorph, fenpropidin, spiroxamine, fenhexamid, fenpyrazamine, piperalin, pyributicarb, naftifine, terbinafine, validamycin, polyoxin, dimethomorph, flumorph, pyrimorph, benthiavalicarb, iprovalicarb, valifenalate, mandipropamid, copper, sulphur, ferbam, mancozeb, maneb, metiram, propineb, thiram, zineb, zinc thiazole, ziram, captan, captafol, folpet, dichlofluanid, tolylfluanid, chlorothalonil, chlozolinate, dimethachlone, anilazine, iprodione, procymidone, vinclozolin, triforine, pyrifenox, pyrisoxazole, fenarimol, guazatine, iminoctadine, dithianon, chinomethionat, quinomethionate, fluoroimide, methasulfocarb, and phenamacril. [0082] As noted herein, the present disclosure includes various forms of the boron- containing compounds, including closed (Formula I), anhydrodimer (Formula II), and open or hydrazone (Formula III), each of which may exist in equilibria with one another depending on various conditions, including but not limited to structure, solvent(s), pH, and temperature. [0083] In some embodiments, as noted herein, compounds of the disclosure may convert to or exist in equilibrium with the other forms described herein. Accordingly, in some embodiments, the compounds described may exist in combination with one or more of these forms. In other embodiments, a certain form may predominate over the other forms due to one or more factors including certain substituent patterns, solvent, pH, and temperature. [0084] Of the three forms (Formula I, Formula II, and Formula III), the present inventors have found that compounds isolated in each form may exhibit differential biological activity compared to the other forms as against potential target pests. There are exceptions. For example, all three forms are herein demonstrated to provide activity against the fungal genus, Botrytis. Therefore, in one embodiment of the present disclosure, the compounds of the present disclosure, in particular the closed form (Formula I) and/or the anhydrodimer form (Formula II), exhibit a broad range of biological activity in that they have antimicrobial properties against several pests when substituted to focus efficacy against a fungal species. In general, the biological activity of the closed and anhydrodimer forms was unanticipated and not predictable based on the open form’s biological activity. In other words, the structure activity relationship does not appear to be extrapolative consistently between the forms. [0085] In another aspect, is a method of reducing, ameliorating, or controlling a plant fungal infestation. That method comprises administering a composition comprising a fungicidally effective amount of a compound of the present disclosure, preferably dissolved or dispersed in a carrier medium to a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables in need thereof. [0086] In one embodiment, the present disclosure includes compositions suitable for treatment of a locus that may be infected with pests, such as a plant, an animal, such as a mammal, or a building, or for the prevention of infection or infestation of such a locus with pests. [0087] In some embodiments of the disclosure, a contemplated compound or a composition containing a contemplated compound is administered locally to an animal or a part of an animal, a plant, a plant parts plant propagation material, and/or harvested fruits or vegetables. In some embodiments, the administration is systemic. [0088] In some embodiments, the administration of a compound or a composition of the disclosure is topical, to the soil, foliar, a foliar spray, systemic, a seed coating, a seed treatment, a soil drench, directly in-furrow dipping, drenching, soil drenching, spraying, atomizing, irrigating, evaporating, dusting, fogging, broadcasting, foaming, painting, spreading-on, watering (drenching), or drip irrigating, or any combinations thereof. [0089] The formulations/agrochemical compositions described herein may comprise a carrier and may be conveniently formulated in a known manner into emulsifiable concentrates, suspension concentrates, coatable pastes, directly sprayable or dilutable solutions, emulsions, wettable powders, soluble powders, dusts, granulates, and/or encapsulations in polymeric substances. The carrier can be any solid carrier or a liquid carrier known in the art suitable for agrochemical compositions. The type of the compositions and the methods of applications such as spraying, atomizing, dusting, scattering, coating or pouring, are chosen based on objectives and the circumstances. A contemplated composition can contain adjuvants such as stabilizers, antifoams, viscosity regulators, binders, or tackifiers, fertilizers, micronutrient donors, additives that enhance plant uptake, spreaders, stickers, or other compositions for obtaining special effects. Such adjuvants can be included in the agrochemical composition/formulation or tank mixed with the agrochemical composition/formulation prior to application. [0090] The preceding is a simplified summary to provide an introduction and understanding of some embodiments of the present disclosure. This summary is neither an extensive nor exhaustive over-view of the present disclosure and its various embodiments. The summary presents selected concepts of the embodiments of the present disclosure in a simplified form as an introduction to the more detailed description presented below. As will be appreciated, other embodiments of the present disclosure are possible utilizing, alone or in combination, one or more of the features set forth above or described in detail below. [0091] The headings used herein are for organizational purposes only and are not meant to be used to limit the scope of the description or the claims. The words “include”, “including”, and “includes” mean including but not limited to the recited description. DEFINITIONS [0092] Any reference in the specification to “one embodiment” or “an embodiment” or “another embodiment” or a similar phrase means that a particular feature, structure, characteristic, operation, or function being described is included in at least one embodiment. Thus, any appearance of the phrases “in one embodiment” or “in an embodiment” in the specification is not necessarily referring to the same embodiment. Further, the particular features, structures, characteristics, operations, or functions may be combined in any suitable manner in one or more embodiments, and it is intended that embodiments of the described subject matter can and do cover modifications and variations of the described embodiments. Particular aspects, as used herein, should be treated in a similar manner. [0093] The phrases “at least one”, “one or more”, and “and/or” are open-ended expressions that are both conjunctive and disjunctive in operation. For example, each of the expressions “at least one of A, B, and C”, “at least one of A, B, or C”, “one or more of A, B, and C”, “one or more of A, B, or C” and “A, B, and/or C” means A alone, B alone, C alone, A and B together, A and C together, B and C together, or A, B, and C together. [0094] The term “a” or “an” entity refers to one or more of that entity. As such, the terms “a” (or “an”), “one or more” and “at least one” may be used interchangeably herein. It is also to be noted that the terms “comprising”, “including”, and “having” may be used interchangeably. [0095] A compound of this disclosure includes those described generally above, and are further illustrated by the classes, subclasses, and species disclosed herein. As used herein, the following definitions shall apply unless otherwise indicated. For purposes of this disclosure, the chemical elements are identified in accordance with the Periodic Table of the Elements, CAS version, “Handbook of Chemistry and Physics”, 75th Ed., CRC Press, New York,NY (1995). Additionally, general principles of organic chemistry are described in "Organic Chemistry", Thomas Sorrell, University Science Books, Sausalito, CA (1999), and "March's Advanced Organic Chemistry", 5th Ed., Ed.: Smith, M.B. and March, J., John Wiley & Sons, New York, NY (2001), “Plant Pathology”, 5 ^th Ed., Gore N Agrios, Elsevier Academic Press, Cambridge, MA (2005), the entire contents of which are hereby incorporated by reference. [0096] The term “hydrocarbyl” refers to a monovalent moiety formed by removing a hydrogen atom from a hydrocarbon. The term ‘hydrocarbyl’ includes alkyl groups, alkenyl groups, and alkynyl groups. A preferred “hydrocarbyl” group is an “alkyl” group. Representative hydrocarbyl groups are alkyl groups having 1 to 25 carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl, nonyl, undecyl, decyl, dodecyl, octadecyl, nonadecyl, eicosyl, heneicosyl, docosyl, and tricosyl, and the isomeric forms thereof such as iso-propyl, t-butyl, iso- butyl, sec-butyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, 1- methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2- dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethyl-butyl; alkenyl groups having 2 to 25 carbon atoms, such as methenyl, ethenyl, 1-propenyl, 2-propenyl, iso-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, iso-butenyl, sec-butenyl, 1-pentenyl, 2-pentenyl, 3- pentenyl, 4-pentenyl, hexenyl, heptenyl, octenyl and the isomeric forms thereof; alkynyl groups having 2 to 25 carbon atoms, such as ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3- butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, hexynyl, pentynyl, and octynyl, and the isomeric forms thereof. A hydrocarbyl group may also be substituted with a “cyclohydrocarbyl” group. Accordingly, groups such as 2-(cyclopropyl)-ethyl, cyclohexylmethyl, cyclopropylethyl, and cyclopropylmethyl, are contemplated hydrocarbyl groups. [0097] In some embodiments, a “hydrocarbyl group” contains 1 to 6 members (C ₁ -C ₆ ). In other embodiments, the hydrocarbyl radical contains 1 to 3 members (C ₁ -C ₃ ). In yet other embodiments, the hydrocarbyl radical may contain from 1 to 17 substitutions, or in another embodiment from 1 to 5 substitutions. The hydrocarbyl group may also contain one or more substituents. [0090] The term “cyclohydrocarbyl”, by itself or part of another substituent, unless otherwise stated, refers to a cyclic hydrocarbyl group which may be fully saturated, monounsaturated, or polyunsaturated and includes C3-C15 hydrocarbons in a ring system. The cyclohydrocarbyl group may contain one or more substituents. In one embodiment, the ring contains 3 to 6 members (C ₃ -C ₆ ). [0091] In another embodiment, a cyclohydrocarbyl group may have from 1 to 11 substitutions, or in another embodiment from 2 to 6 substitutions. Examples of cyclohydrocarbyl groups include, but are not limited to cyclopropyl, cyclopentyl, cyclohexyl, cyclohex-1-enyl, cyclohex-3- enyl, cycloheptyl, cyclooctyl, norbornyl, decalinyl, adamant-1-yl, adamant-2-yl, bicyclo[2.1.0]pentyl, bicyclo[3.1.0]-hexyl, spiro[2.4]heptyl, spiro[2.5]octyl, bicyclo-[5.1.0]octyl, spiro[2.6]nonyl, bicyclo[2.2.0]hexyl, spiro[3.3]heptyl, bicyclo[4.2.0]octyl, and spiro[3.5]nonyl, and the like. [0092] Usual chemical suffix nomenclature is followed when using the word "hydrocarbyl" except that the usual practice of removing the terminal "yl" and adding an appropriate suffix is not always followed because of the possible similarity of a resulting name to one or more substituents. Thus, a hydrocarbyl ether is referred to as a "hydrocarbyloxy" group rather than a "hydrocarboxy" group as may possibly be more proper when following the usual rules of chemical nomenclature. Illustrative hydrocarbyloxy groups include methoxy, ethoxy, n-propoxy, iso-propoxy, allyloxy, n-butoxy, iso-butoxy, sec-butoxy, and tert-butoxy groups. Preferred members of this group are “alkoxy” groups that are illustrated by methoxy, ethoxy, n-propoxy, iso-propoxy, n-butoxy, tert-butoxy, pentoxy, hexoxy, heptoxy, and the like. [0093] A (C ₁ -C ₇ )hydrocarboyl [acyl; -C(O)-(C ₁ -C ₆ )hydrocarboyl] group is a hydrocarbyl residue that is bonded to a carbonyl group that is itself bonded to another substituent. Illustrative (C ₁ - C ₇ )hydrocarboyl groups include formyl, acetyl, propionyl, benzoyl, acryloyl, methacryloyl, cyclopentylcarbonyl, hexanoyl, and the like. [0094] A (C ₁ -C ₇ ) hydrocarboyloxy group is a hydrocarbyl residue that may contain one to seven carbon atoms, i.e.; a (C ₁ -C ₆ )carboxylate ester [-O–C(O)(C ₁ -C ₆ ) hydrocarbyl or -C(O)-O-(C ₁ -C ₆ hydrocarbyl)]. Illustrative (C ₁ -C ₇ )hydrocarboyloxy groups include formyloxy, acetoxy, propionoxy, benzoyloxy, acryloyloxy, hexanoyloxy, and the like. [0095] The term "aryl", unless otherwise stated, used alone or as part of a larger moiety as in “arylalkyl”, is an aromatic, hydrocarbyl group that is monocyclic or polycyclic containing up to three fused rings, and preferably up to two fused rings. Examples of aryl groups include, but are not limited to phenyl, naphthyl, anthracenyl, and phenanthryl and substituted phenyl, naphthyl, anthracenyl, and phenanthryl groups. [0096] Phenyl, naphthyl, and substituted phenyl, and substituted naphthyl groups are preferred aryl groups, with phenyl and substituted phenyl groups being more preferred. In one embodiment, the ring system may have 1 to about 5 substituents, or in another embodiment 2 to 3 substituents are present on the ring system. In one embodiment, the ring system has 1 substituent. [0097] The term “phenyl” as used herein is a C6H5 group. The term “phenyl” may be abbreviated herein as “Ph”. “Phenyl” groups may be substituted. Similarly, the term “naphthyl” as used herein is a C10H7 group. “Naphthyl” groups may be substituted. [0098] The term "heteroaryl", unless otherwise stated, used alone or as part of a larger or smaller moiety as in “aryl”, contain from one to four heteroatoms selected from nitrogen, oxygen, and sulfur, where the nitrogen and sulfur atoms are optionally oxidized, and one or several nitrogen atoms are optionally quaternized. A heteroaryl group may be attached to the remainder of the molecule through a heteroatom. [0099] A heteroaryl group may contain one ring or two fused rings. Non-limiting examples of heteroaryl groups include, 1-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl, 3-pyrazolyl, 1-imidizoyl, 2-imidazolyl, 4-imidazolyl, pyrazinyl, 2-oxazolyl, 4-oxazolyl, 2-phenyl-4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4- isoxazolyl, 5-isoxazolyl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2- pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-benzo-thiazolyl, purinyl, 2-benzimidazolyl, 5-indolyl, 1-isoquinolyl, 5-isoquinolyl, 2-quinoxalinyl, 5-quinoxalinyl, 3-quinolyl, and 6-quinolyl. In one embodiment, examples of heteroaryl groups include pyridine, purine, thiophene, thiazole, imidazole, benzimidazole, pyrazole, 1,2,3- and 1,2,4-triazole, oxazole. In one embodiment, examples of heteroaryl groups include pyridine, thiophene, thiazole, imidazole, benzimidazole, pyrazole, and oxazole. [0100] The terms "arylalkyl" and "heteroarylalkyl" is meant to include those radicals in which an aryl or heteroaryl group is attached to an alkyl group (e.g., benzyl, phenethyl, pyridylmethyl, and the like) including those alkyl groups in which a carbon atom (e.g., a methylene group) has been replaced by, for example, an oxygen atom (e.g., phenoxymethyl, pyrid-2-yloxymethyl, 3-(naphth- 1-yloxy)propyl, and the like). The term “benzyl” as used herein is a radical in which a phenyl group is attached to a CH2 group (i.e. a CH2Ph group). The term substituted benzyl refers to radicals in which the phenyl group contains one or more substituents. In one embodiment, the phenyl group may have 1 to 5 substituents, or in another embodiment 2 to 3 substituents. [0101] Each of the above terms "hydrocarbyl", "cyclohydrocarbyl", "alkoxy", "aryl", "heteroaryl", "arylalkyl", and "heteroarylalkyl" may be present in substituted and unsubstituted forms of the indicated radical unless otherwise stated. The "hydrocarbyl", "cyclohydrocarbyl", "alkoxy", "aryl", "heteroaryl", "arylalkyl", and "heteroarylalkyl" groups are optionally substituted by one or more groups that may be the same or different and which are, independently, selected from halogen such as fluoro, chloro, bromo or iodo and may be mono-, partially substituted or completely substituted (e.g., in the form of -CF ₃ , -CF ₂ CF ₃ , -CHF2, -CH ₂ F, and the like), -R', -OR', -OH, -SH, -SR', - NO ₂ , -CN, -C(O)R', -C(O)OR', -OC(O)R',-CON(R') ₂ , or -OC(O)N(R') ₂ , -NH ₂ , - NHR', -N(R') ₂ , -NHCOR', -NHCOH, -NHCONH ₂ , -NHCONHR', -NHCON(R') ₂ , -NRCOR', - NRCOH, -NHCO ₂ H, -NHCO ₂ R', -CO ₂ R', -CO ₂ H, -CHO, -CONH ₂ , -CONHR',-CON(R') ₂ , -S(O) ₂ H, -S(O) ₂ R', -SO ₂ NH ₂ , -S(O)H, -S(O)R', -SO ₂ NHR', -SO ₂ N(R') ₂ , -NHS(O) ₂ H, -NR'S(O) ₂ H, - NHS(O) ₂ R', -NR'S(O) ₂ R', and -Si(R')3; and where a saturated carbon atom of said "hydrocarbyl", "cyclohydrocarbyl", "alkoxy", "aryl", "heteroaryl", "arylalkyl", or "heteroarylalkyl" groups is optionally substituted with one or more groups that may be the same or different and which are, independently, selected from =O, =S, =NNHR', =NNH ₂ , =NN(R') ₂ , =N-OR', =N-OH, =NNHCOR', =NNHCOH, =NNHCO ₂ R', =NNHCO ₂ H, =NNHSO ₂ R', =NNHSO ₂ H, =N-CN, =NH, or =NR'; and where each occurrence of R' is, independently, selected from "hydrocarbyl", "cyclohydrocarbyl", "alkoxy", "aryl", "heteroaryl", "arylalkyl", and "heteroarylalkyl”. [0102] As used herein, the term "heteroatom" is meant to include oxygen (O), nitrogen (N), and sulfur (S). Heteroatoms oxygen and nitrogen are preferred. [0103] The phrases “independently selected”, “independently” and their variants, when used in reference to two or more of the same substituent group are used herein to mean that that two or more groups may be the same or different. In addition, where one or more substituent positions are recited for such substituent(s), the position numbers and recited substituents(s) take precedence over “independently”. [0104] The term “partially halogenated hydrocarbyl” group means a hydrocarbyl group in which some but not all hydrogens are replaced by a halogen. Illustrative partially fluorinated hydrocarbyl groups include difluoromethyl, 6,6,6-trifluorohexyl, and 2,3,-difluoropropyl. The term “fully halogenated hydrocarbyl” means a hydrocarbyl group wherein each hydrogen has been replaced by a halogen. Examples of such fully halogenated hydrocarbyl groups are perfluorohydrocarbyl groups such as trifluoromethyl, perfluorobutyl, perfluoroisopropyl, and perfluorohexyl. Preferred partially and fully halogenated hydrocarbyl groups are partially and fully fluorinated hydrocarbyl groups and partially and fully chlorinated hydrocarbyl groups. [0105] The terms “pathogen” and “pest” are used interchangeably herein to broadly include any organism that may be harmful to the entity to which a contemplated compound or composition containing such a compound is administered. The term “pest” includes plant and animal pests. A “pathogen” or “pest” is intended to include a microbe, an insect, an arachnid, or a parasite, or other organism that may cause infection or disease directly or as a vector, as well as any combinations thereof. Plant pests are commonly nematodes, insects, arachnids, bacteria, viruses, or fungi, or combinations thereof. Animal pathogens or pests include similar types of pests, but usually do not include nematodes and do include helminths. Insect and arachnid pests of plants often eat one or more portions of a plant, plant parts, plant propagation materials, and/or harvested fruits or vegetables. Additionally, biting insects are often pests in and of themselves, but may also be vectors for microbially-caused diseases such as malaria, plague, and Lyme disease. [0106] “Phytopathogen” as used herein, is a pathogen affecting a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables. Plant pathogens are commonly insects, arachnids, parasites, or microbes, or combinations thereof. Insect pests of plants often eat or suck fluids from one or more portions of a plant. [0107] The phrase “True Fungi” is used herein means all members of the kingdom Fungi, including, but not limited to, yeasts, rusts, smuts, mildews, molds, and mushrooms, excepting members of Oomycota (Phytophthora infestens and Plasmopara viticola). The term “fungi” or “fungus” is used to include all of the fungal organisms discussed herein, including the Oomycota. [0108] The term “plant health” generally describes various sorts of characteristics of plants. For example, properties that may be mentioned are crop characteristics including: emergence, crop yields, protein content, oil content, starch content, root system, root growth, root size maintenance, stress tolerance (e.g. against drought, heat, salt, UV, water, cold), ethylene (production and/or reception), tillering, plant height, leaf blade size, number of basal leaves, tillers strength, leaf color, pigment content, photosynthetic activity, amount of input needed (such as fertilizers or water), seeds needed, tiller productivity, time to flowering, time to grain maturity, plant verse (lodging), shoot growth, plant vigor, plant stand, tolerance to biotic and abiotic stresses, natural defense mechanisms, and time to germination. [0109] In general, “pesticidal” means the ability of a substance to increase mortality or inhibit the growth rate of plant and/or animal pests. The term is used herein, to describe the property of a substance to exhibit activity against microbes, insects, arachnids, parasites, and/or other pests. A substance that is pesticidal is a “pesticide”. [0110] The term ‘active agent’ or ‘active ingredient’ or ‘active compound’ means a contemplated compound. [0111] By “effective” amount of a drug, active ingredient, pesticide, fungicide, nematicide, arachnicide, antiparasitic, antimicrobial, insecticide, formulation, composition, or permeant is meant a sufficient amount of an active agent to provide the desired local or systemic effect. A(n) “effective”, “topically effective”, “therapeutically effective”, “fungicidally effective”, “nematicidally effective”, “antimicrobially effective”, “arachnicidally effective”, or “insecticidally effective” amount refers to the amount of drug needed to effect the desired biological result. [0112] The term “control” or “controlling” refers to a composition that provides a curative and/or inhibitive activity of pests. [0113] The term “composition” includes stereoisomers and agriculturally, pesticidally, or veterinary acceptable salts of the active agents disclosed herein. The compound of the disclosure included in the composition may be covalently attached to a carrier moiety, as described herein. Alternatively, any compound of the disclosure included in the composition is not covalently linked to a carrier moiety. [0114] The terms “acceptable salt”, “pharmaceutically (or veterinary) acceptable salt” and “agriculturally acceptable salt” are meant to include a salt of a compound of the disclosure which are prepared with relatively nontoxic acids or bases, depending on the particular substituents found on the compounds described herein. When compounds of the disclosure contain relatively acidic functionalities, base addition salts may be obtained by contacting the neutral form of such compounds with a sufficient amount of the desired base, either neat or in a suitable inert carrier. Examples of agriculturally acceptable base addition salts include sodium, potassium, zinc, calcium, ammonium, organic amino (such as choline or diethylamine or amino acids such as d-arginine, l-arginine, d-lysine, or l-lysine), or magnesium salt, or a similar salt. When compounds of the disclosure contain relatively basic functionalities, acid addition salts may be obtained by contacting the neutral form of such compounds with a sufficient amount of the desired acid, either neat or in a suitable inert solvent. Examples of pharmaceutically acceptable acid addition salts include those derived from inorganic acids like hydrochloric, hydrobromic, nitric, carbonic, monohydrogencarbonic, phosphoric, monohydrogen-phosphoric, dihydrogenphosphoric, sulfuric, monohydrogensulfuric, hydriodic, or phosphorous acids and the like, as well as the salts derived from relatively nontoxic organic acids like acetic, propionic, isobutyric, maleic, malonic, benzoic, succinic, suberic, fumaric, lactic, mandelic, phthalic, benzenesulfonic, p-tolylsulfonic, citric, tartaric, methanesulfonic, and the like. Also included are salts of amino acids such as arginate and the like, and salts of organic acids like glucuronic or galactunoric acids and the like (see, for example, Berge et al., “Pharmaceutical Salts”, J Pharm Sci 66:1-19 (1977)). Certain specific compounds of the disclosure contain both basic and acidic functionalities that allow the compounds to be converted into either base or acid addition salts. [0115] The term “acceptable carrier” or “acceptable vehicle” refers to any medium that provides the appropriate delivery of an effective amount of an active agent(s), fungicide, nematicide, insecticide, drug, formulation, or permeant, as defined herein, does not negatively interfere with the effectiveness of the biological activity of the active agent, fungicide, nematicide, insecticide, drug, formulation, or permeant, and that is sufficiently non-toxic to the host, whether agricultural, pharmaceutical, veterinary, or pesticidal to a locus that may be infected with pests, such as a plant, an animal, such as a mammal, or a building, or for the prevention of infection or infestation of such a locus with pests. [0116] Representative carriers include water, oils, both vegetable and mineral, cream bases, lotion bases, emulsion bases, ointment bases and the like. These bases include suspending agents, thickeners, penetration enhancers, and the like. Additional information concerning carriers may be found in Remington: The Science and Practice of Pharmacy, 21st Ed., Lippincott, Williams & Wilkins (2005), which is incorporated herein by reference. [0117] The term "carrier" is used herein to denote a natural or synthetic, organic, or inorganic material that constitutes a portion of the diluent medium in which the active agent is dispersed or dissolved. This carrier is inert. In some embodiments, this carrier is inert and agriculturally acceptable, in particular to the plant being treated. The phrase “agriculturally acceptable” is utilized herein to be analogous to “pharmaceutically acceptable” as used in pharmaceutical products to describe diluent media. A carrier may be solid (clays, natural or synthetic silicates, silica, resins, waxes, solid fertilizers, dusts and dispersible powders such as kaolinite, lactose, calcite, talc, kaolin, bentonite, or other absorptive polymers, and the like) or liquid (water, alcohols, ketones, petroleum fractions, aromatic or paraffinic hydrocarbons, chlorinated hydrocarbons, liquefied gases, and the like). [0118] The term “acceptable excipient” is conventionally known to mean agriculturally acceptable carriers, agriculturally acceptable diluents and/or agriculturally acceptable vehicles used in formulating compositions effective for the desired use. [0119] “Pharmaceutical compositions” includes stereoisomers and pharmaceutically acceptable salts of the active agents disclosed herein. The compound of the disclosure included in the composition may be covalently attached to a carrier moiety. Alternatively, any of the compounds of the disclosure included in the composition is not covalently linked to a carrier moiety. [0120] “Agrochemical compositions” includes stereoisomers and agrochemically acceptable salts of the active agents disclosed herein. The compound of the disclosure included in the composition may be covalently attached to a carrier moiety. Alternatively, any of the compounds of the disclosure included in the composition is not covalently linked to a carrier moiety. [0121] An " acceptable carrier," as used herein refers to excipients, for example, pharmaceutically, veterinary, or physiologically, acceptable organic or inorganic carrier substances suitable for enteral or parenteral application that do not deleteriously react with the active agent. Suitable acceptable carriers include water, salt solutions (such as Ringer's solution), alcohols, oils, gelatins, and carbohydrates such as lactose, amylose or starch, fatty acid esters, hydroxymethycellulose, and polyvinyl pyrrolidine. Such preparations may be sterilized and, if desired, mixed with auxiliary agents such as lubricants, preservatives, stabilizers, wetting agents, emulsifiers, salts for influencing osmotic pressure, buffers, coloring, and/or aromatic substances and the like that do not deleteriously react with the compounds of the disclosure. [0122] The term “microbe” is intended to include any microscopic organism that is harmful to the entity to which a contemplated compound or composition containing such is administered. The term “microbe” is intended to include fungi, bacteria, and viruses, as well as any combinations thereof. The term “microbe” includes all bacteria, fungi, and viruses. In one embodiment, the term is limited to fungi. In one embodiment, the compounds of the present disclosure provide broad spectrum anti-fungal activity. [0123] The term “antimicrobial” means a compound that reduces, ameliorates, or controls the growth of microbes. [0124] “Fungicide” and “fungicidal” refers to the ability of a substance to reduce, ameliorate, or control the growth rate of fungi. [0125] The term “parasite” as used herein is intended to include protozoa, parasitic worms, helminths, trematodes, nematodes, flatworms, and endoparasities that are harmful to plants or animals. [0126] The term “antiparasitic” means a compound that reduces, ameliorates, or controls the growth of parasites. [0127] “Nematicides” and “nematicidal” refers to the ability of a substance to reduce, ameliorate, or control the growth of nematodes. In general, the term “nematode” comprises eggs, larvae, juvenile, and mature forms of said organism. [0128] “Insecticide” as well as the term “insecticidal” refers to the ability of a substance to reduce, ameliorate, or control the growth of insects. As used herein, the term “insects” includes all organisms in the class “Insecta.” The term “pre-adult” refers to any form of an organism prior to the adult stage, including, for example, eggs, larvae, instars, and nymphs. [0129] Arachnicides including “acaricides” and “acaricidals” refer to the ability of a substance to reduce, ameliorate, or control the growth of ectoparasites belonging to the class “Arachnida”, and particularly sub-class Acari. The term “pre-adult” refers to any form of an organism prior to the adult stage, including, for example, eggs, larvae, instars, and nymphs. [0130] The term “vigor” is the measure of the increase in plant growth or foliage volume through time after planting. [0131] The term “animal” generally includes commercial animals, livestock, companion animals, wild animals, and humans. In some embodiments, for any of the methods described herein, the animal is a mammal. In some embodiments, a mammal is a member selected from human, cattle, deer, reindeer, goat, honey bee, pig, sheep, horse, cow, bull, dog, guinea pig, gerbil, rabbit, cat, camel, yak, elephant, ostrich, otter, chicken, duck, goose, guinea fowl, pigeon, swan, and turkey. In some embodiments, for any of the methods described herein, a mammal is a human. [0132] The term “animal health” generally means the achievement and maintenance of healthful homeostasis of an animal, whether the animal be commercial, livestock, companion animal, wild, or human. [0133] “Biological medium,” as used herein refers to both in vitro and in vivo biological milieus. Exemplary in vitro “biological media” include, but are not limited to, cell culture, tissue culture, homogenates, plasma, and blood. In vivo applications may be performed in animals and plants. Additionally, unless otherwise stated, structures depicted herein are also meant to include compounds that differ only in the presence of one or more isotopically enriched atoms. [0134] For example, compounds having the present structures including the replacement of hydrogen by deuterium or tritium, or the replacement of a carbon by a ¹³ C- or ¹⁴ C-enriched carbon are within the scope of this disclosure. Such compounds are useful, for example, as analytical tools, as probes in biological assays, or as therapeutic agents in accordance with the present disclosure. BRIEF DESCRIPTION OF THE DRAWINGS [0135] Figures 1a and 1b are each Tables, providing results of biological testing for compounds of the present disclosure, including activity against several fungi. In light of taxonomical updating, reference to Alternaria solani in Figures 1a and 1b may also be considered as a reference to Alternaria linariae. [0136] Figure 2 is a Table, providing results of biological testing for compounds of the present disclosure, including activity against several fungi. [0137] Figure 3 ilustrates the impact of compounds of the present disclosure on nematode motility relative to average motility of untreated nematodes, provided as percent mortality data sets as herein described in further detail, thereby rendering EC50 values. DETAILED DESCRIPTION [0138] The description set forth below is intended as a description of various embodiments of the described subject matter and is not necessarily intended to represent the only embodiment(s). In certain instances, the description includes specific details for the purpose of providing an understanding of the described subject matter. However, it will be apparent to those skilled in the art that embodiments may be practiced without the specific details as described. Contemplated Compounds of the Disclosure [0139] In one aspect, the present disclosure contemplates Compound List A. In one aspect, the present disclosure contemplates Compound List B. In one aspect, the present disclosure contemplates Compound List C. In one aspect, the present disclosure contemplates Compound List D. In one aspect, the present disclosure contemplates Compound List E. In one aspect, the present disclosure contemplates Compound List F. In one aspect, the present disclosure contemplates Compound List G. [0140] In yet other embodiments, a contemplated compound is selected from one or more of the Compound Lists, shown in one structural form, but appreciating the other structural forms. [0141] It is to be understood that when in aqueous media, some contemplated compounds of Formula I where Y is O as illustrated may be present in a reversible equilibrium with water due the Lewis acidic nature of the trigonal planar boron center (e.g., compounds shown below). This dynamic equilibrium can be important for the biological activity of the compounds of the present disclosure. All compounds in the present disclosure in this dynamic equilibrium are another aspect of the present disclosure. [0142] As noted previously, the inventors have found that the different forms offer different biological activity. There are exceptions where the three forms offer similar activity. For example, the open form (Formula III) is particularly effective against the fungal genus pest Botrytis and particularly B. cinerea, thus exhibiting specificity in biological action. As a consequence, one form, such as an open form compound of Formula III, may not be contemplated as a broad spectrum fungicide, but may neverhtelss be useful against Botrytis, while sparing other possible pests. A particularly preferred contemplated compound of this aspect is one or more of Compound List D. [0143] Accordingly, for some of the compounds disclosed herein, an open form of a contemplated compound could be present along with the closed and/or anhydrodimeric forms, together forming a pesticidal composition. For some compounds of the disclosure, one form predominates under particular conditions. [0144] In some embodiments of the present disclosure, the closed form was found to unexpectedly have a broad biologic activity against a plurality of pathogens. Accordingly, the data presented herein demonstrate that compounds of Formula I, Formula II, and Formula III, particularly Formula I and Formula III, may be considered distinct chemical matter. [0145] For the compounds disclosed herein, because of the existence of the anionic hydrate forms, such compounds may exist as a salt when combined with an appropriate cation. Illustrative appropriate cations are well known and include monovalent alkali metal cations, sodium, and potassium, alkaline earth cations such as magnesium, calcium and barium, as well as other metal salts such as iron, manganese, cobalt, and the like. Ammonium cations may also be used such as an ammonium group, C ₁ -C ₆ mono- and diamines and their C ₁ -C ₃ mono-, di-, tri- and tetraalkyl and and benzyl ammonium ions. A suitable listing of pharmaceutically useful cations that may be utilized herein may be found in Berge et al., J Pharm Sci 66(1):1-19 (1977). [0146] A suitable salt form may be prepared by passage of an aqueous solution of a contemplated compound through as ion exchange resin containing a desired cation. Once prepared, the formula for the resulting salt contains a M+ symbol rather than the H+ shown above to indicate the presence of a cation other than hydronium. Methods of Use [0147] In one embodiment, a method is provided for promoting plant performance and/or reducing, ameliorating, or controlling an infestation of a pest (e.g. microbes, insects, arachnids, and/or parasites) on or in an animal, a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables by administering a compound or a composition according to the disclosure as described herein. [0148] Thus, a method of reducing, ameliorating, or controlling an infestation of a pest is contemplated. That method comprises administering a composition comprising Compound List A, B, C, D, E, F, or G. [0149] Although a compound contemplated for use herein may be useful in treating one or more plant and/or animal pests, the present compounds are useful as antimicrobials, particularly in treating fungal infections, and more particularly, fungal infections of plants. The compounds of the present disclosure are believed to exhibit broad spectrum anti-fungal effects. [0150] Preferably, a compound used in the above method is a compound of Formula I, II, or III and most preferably, the contemplated compound utilized in this method is a compound whose structural formula is shown in Compound List A, Compound List B, Compound List C, Compound List D, Compound List E, Compound List F, or Compound List G. [0151] In yet other embodiments, a contemplated compound useful in the above-discussed method, particularly as a fungicide, and is selected from one or more of those of the compounds disclosed in Compound List A, Compound List B, Compound List C, Compound List D, Compound List E, Compound List F, and Compound List G (or an alternative structural form of such a compound). [0152] As noted before, an open form of a contemplated compound (Formula III) may or may not be generally active against the broad range of pests similar to the range of activity encompassed by a compound of Formula I or Formula II. Rather, a contemplated compound of Formula III may show selective activity, and, therefore, may be useful for reducing, ameliorating, or controlling a fungal infestation of a certain genus, such as, for example, the genus Botrytis. Accordingly, and as noted herein, in another aspect, the present disclosure provides a method of reducing, ameliorating, or controlling a plant fungal infestation by the genus Botrytis, and particularly B. cinera. That method comprises administering a composition comprising a fungicidally effective amount of a compound, dissolved or dispersed in a carrier medium to a plant in need thereof. [0153] It is to be understood that a compound of Formula III may exist as stereoisomers in a syn and/or anti form (or cis and/or trans form), as is the case in many so-called third generation cephalosporin compound oxime hydroxyl-protected groups of cefepime, cefpirome and ceftazidime. Both the syn and anti stereoisomeric forms are contemplated herein. [0154] A contemplated compound may be used in antimicrobial, insecticidal, arachnicidal, and/or parasiticidal compositions for controlling or protecting against phytopathogens, where the composition comprises as an active agent of at least one compound of the Formulae of the present disclosure. [0155] The presence of one or more possible asymmetric centers in a compound of the disclosure means that the compounds may occur in chiral isomeric forms, i.e., enantiomeric or diastereomeric forms. In some embodiments, a boron may be an asymmetric center. Also, atropisomers may occur as a result of restricted rotation about a single bond. The disclosed compound formulas are intended to include all those possible isomeric forms and mixtures thereof. The present disclosure includes all those possible isomeric forms and mixtures thereof for compounds of the disclosed disclosure. The disclosed compounds are intended to include all possible tautomers (e.g. keto-enol tautomerism) where present. Accordingly, the present disclosure includes all possible tautomeric forms for the disclosed compounds. [0156] Some embodiments provide a method for reducing, ameliorating, or controlling an infestation by a pathogen by applying a compound or a composition of the present disclosure, wherein the pathogen is a microbe, an insect, an arachnid, a parasite, or any combinations thereof. [0157] In other embodiments, the compounds of the present disclosure are applied to an animal, a plant, a plant part, a plant propagation material, or another locus, including but not limited to soil or a building where infestation occurs. [0158] In other embodiments of the disclosure, the pathogen is a phytopathogenic. [0159] In yet other embodiments, compounds or the compositions of the present disclosure may be applied topically, to the soil, foliar, a foliar spray, systemic, a seed coating, a seed treatment, a soil drench, directly in-furrow dipping, drenching, soil drenching, spraying, atomizing, irrigating, evaporating, dusting, fogging, broadcasting, foaming, painting, spreading- on, watering (drenching), and drip irrigating, or any combinations thereof. Agrochemical Compositions [0160] A contemplated compound may be used in unmodified form or together with one or more carriers conventionally employed in the art of formulation. A contemplated compound may be prepared as a formulation that is an agrochemical composition. They may be formulated into emulsifiable concentrates, suspension concentrates, water dispersible concentrates, coatable pastes, directly sprayable, or dilutable solutions or suspensions, dilute emulsions, wettable powders, water-dispersible granules, soluble powders, dusts, granulates, seed treatments, and also encapsulations e.g., in polymeric substances. The methods of application, such as spraying, atomizing, dusting, scattering, coating, or pouring, are chosen in accordance with the intended objectives and the prevailing circumstances. Also contemplated in the present disclosure are conventional slow release formulations. [0161] The compositions may also contain further adjuvants such as stabilizers, antifoams, viscosity regulators, binders, or tackifiers, as well as fertilizers, micronutrient donors, or other formulations for obtaining the intended effect(s). They may also contain surfactants (also known as surface-active agents). [0162] Suitable surfactants are surface-active compounds, such as anionic, cationic, nonionic and amphoteric surfactants, block polymers, polyelectrolytes, and mixtures thereof. Such surfactants can be used as emulsifier, dispersant, solubilizer, wetter, penetration enhancer, protective col- loid, or adjuvant. Examples of surfactants are listed in McCutcheon's, Vol.1 : Emulsifiers & Detergents, McCutcheon's Directories, Glen Rock, USA, 2008 (International Ed. or North American Ed.). [0163] Suitable anionic surfactants are alkali, alkaline earth or ammonium salts of sulfonates, sulfates, phosphates, carboxylates, and mixtures thereof. Examples of sulfonates are alkylarylsulfonates, diphenylsulfonates, alpha-olefin sulfonates, lignine sulfonates, sulfonates of fatty acids and oils, sulfonates of ethoxylated alkylphenols, sulfonates of alkoxylated arylphenols, sulfonates of condensed naphthalenes, sulfonates of dodecyl- and tridecylbenzenes, sulfonates of naphthalenes and alkylnaphthalenes, sulfosuccinates or sulfosuccinamates. [0164] Examples of sulfates are sulfates of fatty acids and oils, of ethoxylated alkylphenols, of alcohols, of ethoxylated alcohols, or of fatty acid esters. Examples of phosphates are phosphate esters. Examples of carboxylates are alkyl carboxylates, and carboxylated alcohol or alkylphenol ethoxylates. [0165] Suitable nonionic surfactants are alkoxylates, N-subsituted fatty acid amides, amine oxides, es- ters, sugar-based surfactants, polymeric surfactants, and mixtures thereof. Examples of alkoxylates are compounds such as alcohols, alkylphenols, amines, amides, arylphenols, fatty acids or fatty acid esters which have been alkoxylated with 1 to 50 equivalents. Ethylene oxide and/or propylene oxide may be employed for the alkoxylation, preferably ethylene oxide. Examples of N-substituted fatty acid amides are fatty acid glucamides or fatty acid alkanolamides. Examples of esters are fatty acid esters, glycerol esters or monoglycerides. Examples of sugar-based surfactants are sorbitans, ethoxylated sorbitans, sucrose and glucose esters or alkylpolygluco- sides. Examples of polymeric surfactants are home- or copolymers of vinylpyrrolidone, vinylal- cohols, or vinylacetate. [0166] Suitable cationic surfactants are quaternary surfactants, for example quaternary ammonium compounds with one or two hydrophobic groups, or salts of long-chain primary amines. Suitable amphoteric surfactants are alkylbetains and imidazolines. Suitable block polymers are block polymers of the A-B or A-B-A type comprising blocks of polyethylene oxide and polypropylene oxide, or of the A-B-C type comprising alkanol, polyethylene oxide and polypropylene oxide. Suitable polyelectrolytes are polyacids or polybases. Examples of polyacids are alkali salts of poly- acrylic acid or polyacid comb polymers. Examples of polybases are polyvinylamines or polyeth- yleneamines. [0167] Suitable adjuvants are compounds, which have a negligible or even no pesticidal activity themselves, and which improve the biological performance of the active on the target. Examples are surfactants, mineral or vegetable oils, and other auxilaries. Further examples are listed by Knowles, Adjuvants and additives, Agrow Reports DS256, T&F Informa UK, 2006, chapter 5. [0168] Suitable diluent media, carriers and adjuvants (auxiliaries) may be solid or liquid and are substances useful in formulation technology, e.g., natural or regenerated mineral substances, solvents, dispersants, wetting agents, tackifiers, thickeners, binders, or fertilizers. Such diluent media are for example described in WO 97/33890, which is hereby incorporated by reference. Water-based (more than 50 weight percent water) diluent media are used illustratively herein. [0169] Suitable carriers and adjuvants may be solid or liquid or gel, and are substances useful in formulation technology, for example: mineral substances, solvents, dispersants, wetting agents, tackifiers, thickeners, binders, surfactants, and/or fertilizers. [0170] Suitable surface-active compounds are non-ionic, cationic and/or anionic surfactants having good emulsifying, dispersing and wetting properties, depending on the water solubility of the compound of the disclosure. The term “surfactants” is also to be understood as meaning mixtures of two or more surface-active compounds. [0171] The surfactants customarily employed in formulation technology are described, inter alia, in the following publications: McCutcheon's, Vol.1 : Emulsifiers & Detergents, McCutcheon's Directories, Glen Rock, USA, 2008 (International Ed. or North American Ed.).; M. and J. Ash, “Encyclopedia of Surfactants”, Vol. I-III, Chemical Publishing Co., New York, 1980-1981. [0172] In general, a concentrated formulation comprising a contemplated compound includes about 0.01 to about 90% by weight contemplated compound, about 0 to about 20% agriculturally acceptable surfactant and 5 to 99.99% solid or liquid carrier and adjuvant(s). [0173] A formulation as administered preferably comprises about 0.00000001% to about 98% by weight contemplated compound or, with particular preference, about 0.01% to about 95% by weight contemplated compound, more preferably about 0.5% to about 90% by weight contemplated compound. Administration takes place in a customary manner adapted to the application forms. [0174] A contemplated formulation may also include at least one polymer that is a water-soluble or water-dispersible film-forming polymer that improves the adherence of the compound of the disclosure to the plant or plant propagation material. [0175] In some embodiments, a coloring agent, such as a dye or pigment, is included in the agrochemical composition so that an observer may immediately determine that the plant or plant propagation material has been treated. [0176] In typical use, a compound of the disclosure is formulated as a concentrate also known as a pre-mix composition (or concentrate, concentrated formulation, formulated compound, agrochemical composition), and the end user normally employs a diluted formulation for administration to the plants of interest. Such a diluted composition is often referred to as a tank- mix composition. A tank-mix composition is generally prepared by diluting a pre-mix agrochemical composition (concentrate) with a solvent such as water that may optionally also contain further auxiliaries. Generally, an aqueous tank-mix is used. [0177] Particularly, formulations for crop protection may be applied as a spray, e.g., foliar, soil, etc. as are well known in this art. [0178] A contemplated compound may be present in free form, as a hydrate, or as a salt thereof. Pharmaceutical Compositions [0179] A compound of the present disclosure may be prepared and administered in a wide variety of oral, parenteral, and topical dosage forms. Thus, a compound of the present disclosure may be administered by injection (e.g. intravenously, intramuscularly, intracutaneously, subcutaneously, intraduodenally, or intraperitoneally). Also, a compound described herein may be administered by inhalation, for example, intranasally. Additionally, the compounds of the present disclosure may be administered transdermally. It is also envisioned that multiple routes of administration (e.g., intramuscular, oral, transdermal) may be used to administer the compounds of the disclosure. Accordingly, the present disclosure also provides a pharmaceutical composition comprising one or more contemplated compounds dissolved or dispersed in a pharmaceutically acceptable carrier or excipient. [0180] For preparing a pharmaceutical composition from a compound of the present disclosure, pharmaceutically acceptable carriers may be either solid or liquid. Solid form preparations include powders, tablets, pills, capsules, cachets, suppositories, and dispersible granules. A solid carrier may be one or more substances that may also act as diluent, flavoring agent, binder, preservative, tablet disintegrating agent, or an encapsulating material. The contemplated compound may be either in solution, as a dispersion, or as an emulsion. Dispersions may also be prepared, for example, in water, glycerol, liquid polyethylene glycols, and mixtures thereof, and in oils. [0181] In powders, the carrier is a finely divided solid in a mixture with the finely divided active component. In tablets, the active component is mixed with the carrier having the necessary binding properties in suitable proportions and compacted in the shape and size desired. [0182] The powders and tablets preferably contain about 5% to about 70% of the active compound. Suitable carriers are magnesium carbonate, magnesium stearate, talc, sugar, lactose, pectin, dextrin, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose, a low melting wax, cocoa butter, and the like. [0183] The term "preparation" as used herein is intended to include a formulation of the active compound with encapsulating material as a carrier providing a capsule in which the active component with or without other carriers, is surrounded by a carrier, which is thus in association with it. Similarly, cachets and lozenges are included. Tablets, powders, capsules, pills, cachets, and lozenges may be used as solid dosage forms suitable for oral administration. [0184] A pharmaceutical composition comprising an active compound of the presently disclosed subject matter may be manufactured by means of conventional mixing, dissolving, granulating, dragee-making, levigating, emulsifying, encapsulating, entrapping or lyophilization processes. A composition may be formulated in conventional manner using one or more physiologically acceptable carriers, diluents, excipients or auxiliaries which facilitate processing of the active compounds into preparations, which may be used pharmaceutically. [0185] Such a composition also may contain formulating agents, such as suspending, stabilizing and/or dispersing agent. The formulations for injection may be presented in unit dosage form (e.g., in ampules or in multidose containers) and may contain added preservatives. Alternatively, the injectable formulation may be provided in powder form for reconstitution with a suitable vehicle, including but not limited to sterile pyrogen free water, buffer, dextrose solution, and the like, before use. To this end, the active compound(s) may be dried by any art-known technique, such as lyophilization, and reconstituted prior to use. [0186] Liquid preparations for oral administration may take the form of, for example, elixirs, solutions, syrups or suspensions, or they may be presented as a dry product for constitution with water or other suitable vehicle before use. Such liquid preparations may be prepared by conventional means with pharmaceutically acceptable additives such as suspending agents (e.g., sorbitol syrup, cellulose derivatives or hydrogenated edible fats); emulsifying agents (e.g., lecithin or acacia); non aqueous vehicles (e.g., almond oil, oily esters, ethyl alcohol or fractionated vegetable oils); and preservatives (e.g., methyl or propyl p-hydroxy-benzoates or sorbic acid). A preparation also may contain buffer salts, preservatives, flavoring, coloring and sweetening agents as appropriate. [0187] Liquid form preparations include solutions, suspensions, and emulsions, for example, water or water/propylene glycol solutions. For parenteral injection, liquid preparations may be formulated in solution in aqueous polyethylene glycol solution. [0188] Also included are solid form preparations that are intended to be converted, shortly before use, to liquid form preparations for oral administration. Such liquid forms include solutions, suspensions, and emulsions. These preparations may contain, in addition to the active component, colorants, flavors, stabilizers, buffers, artificial and natural sweeteners, dispersants, thickeners, solubilizing agents, and the like. [0189] A pharmaceutical preparation is preferably in unit dosage form. In such form the preparation is subdivided into unit doses containing appropriate quantities of the active component. The unit dosage form may be a packaged preparation, the package containing discrete quantities of preparation, such as packeted tablets, capsules, and powders in vials or ampoules. Also, the unit dosage form may be a capsule, tablet, cachet, or lozenge itself, or it may be the appropriate number of any of these in packaged form. [0190] The quantity of active component in a unit dose preparation may be varied or adjusted from about 0.1 mg to about 10000 mg, more typically about 1.0 mg to about 1000 mg, most typically about 10 mg to about 500 mg, according to the particular application and the potency of the active component. The composition may, if desired, also contain other compatible therapeutic agents. [0191] Some compounds have limited solubility in water and therefore may require a surfactant or other appropriate co-solvent in the composition. Such co-solvents include: Polysorbate® 20, 60, and 80; Pluronic® F-68, F-84, and P-103; cyclodextrin; and polyoxyl 35 castor oil. Such co- solvents are typically employed at a level of about 0.01 % to about 2% by weight. [0192] A viscosity greater than that of water may be desirable to decrease variability in dispensing a formulation, to decrease physical separation of components of a formulated suspension or emulsion of, and/or otherwise to improve a formulation. Such viscosity building agents include, for example, polyvinyl alcohol, polyvinyl pyrrolidone, methyl cellulose, hydroxy propyl methylcellulose, hydroxyethyl cellulose, carboxymethyl cellulose, hydroxy propyl cellulose, chondroitin sulfate and salts thereof, hyaluronic acid and salts thereof, and combinations of the foregoing. Such agents are typically employed at a level of about 0.01% to about 2% by weight. [0193] For prolonged delivery, an active compound(s) or prodrug(s) may be formulated as a depot preparation for administration by implantation or intramuscular injection. The active ingredient may be formulated with suitable polymeric or hydrophobic materials (e.g., as an emulsion in an acceptable oil) or ion exchange resins, or as sparingly soluble derivatives, e.g., as a sparingly soluble salt. [0194] For administration to a non-human animal, the composition containing the therapeutic compound may be added to the animal's feed or drinking water. Also, it may be convenient to formulate animal feed and drinking water products so that the animal takes in an appropriate quantity of the compound in its diet. It may further be convenient to present the compound in a composition as a premix for addition to the feed or drinking water. The composition may also be formulated as a food or drink supplement for humans. Agricultural Activity [0195] In one aspect, the disclosure includes a compound and a method for reducing, ameliorating, or controlling an infestation by a pathogen by applying a compound according to any one of the above formulae, wherein the pathogen is selected from the group consisting of: a microbe, an insect, an arachnid, and a parasite, or any combinations thereof. In some embodiments, the compound is applied in an effective amount. In a preferred embodiment, the microbe is a fungus. [0196] In yet another aspect, the disclosure includes a method for reducing, ameliorating, or controlling an infestation of a pathogen by treating an animal, a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables with a compound according to the compounds of the disclosure. In some embodiments, the compound is applied in an effective amount. In a preferred embodiment, the microbe is a fungus. [0197] In one embodiment of the disclosure, there is provided a composition comprising a compound of the present disclosure. In another aspect, the present disclosure provides agrochemical compositions comprising a contemplated compound in combination with an agrochemically suitable carrier. [0198] In yet another embodiment, an agrochemical composition comprising a contemplated compound dissolved or dispersed in an agrochemically-acceptable diluent or carrier is administered to or on an animal, a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables. [0199] The compounds and compositions disclosed herein provide a method for reducing, ameliorating, or controlling an infestation by a pathogen. The pathogen is selected from a group consisting of: a microbe, an insect, an arachnid, and a parasite, or any combinations thereof. In a preferred embodiment, the microbe is a fungus. [0200] A composition containing a contemplated compound exhibits antipathogenic activity, good plant tolerance, and low toxicity to plants and animals, while exhibiting low environmental impact. [0201] The compositions are suitable for protecting plants, plant parts, plant propagation material, and/or harvested fruits or vegetables; for increasing harvest yields; for improving the quality and/or vigor of the harvested material. [0202] The compositions are suitable for controlling animal pests, in particular microbes, insects, arachnids, and/or parasites such as helminths, nematodes, protozoa, and molluscs that are encountered in agriculture, in horticulture, in animal husbandry, in forests, in gardens and leisure facilities, in protection of stored products and of materials, and in the hygiene sector. [0203] A method of reducing, ameliorating, or controlling a pest such as a microbe, an insect, an arachnid, or a parasite, or any combinations thereof is contemplated. In accordance with that method, the pest is contacted with an effective amount of a contemplated compound described, and that contact is maintained for a period of time sufficient to reduce, ameliorate, and/or control the pest. [0204] For example, that contact is carried out by administering the compounds described herein to the pest where the administration is topical, to the soil, foliar, a foliar spray, systemic, a seed coating, a seed treatment, a soil drench, directly in-furrow dipping, drenching, soil drenching, spraying, atomizing, irrigating, evaporating, dusting, fogging, broadcasting, foaming, painting, spreading-on, watering (drenching), or drip irrigating, or any combinations thereof. In some embodiments, the administration is repeated. [0205] In another aspect of the present disclosure, a compound described herein is used for reducing overall damage of plants and plant parts as well as losses in harvested fruits or vegetables caused by a phytopathogen. [0206] In a further aspect of the present disclosure, the compounds described herein are employed to reduce infection in plants caused by fungi, bacteria, insects, or nematodes. [0207] Furthermore, in another aspect, the compounds described herein, increase the overall plant health. [0208] Moreover, in yet another aspect, the compounds described herein, increase overall animal health. [0209] The good pesticidal activity of the compounds according to the disclosure corresponds to a mortality rate of at least 50-60% of the pests mentioned, more preferably to a mortality rate over 90%, most preferably above 90%, above 91%, above 92%, above 93%, about 94%, above 95%, above 96%, above 97%, above 98%, above 99%, or 100%. [0210] The compositions herein disclosed, in some embodiments, are active against normally sensitive and resistant species and against all or some stages of development. [0211] Furthermore, a contemplated compound may have potent activity and may be used for control of unwanted pathogens (particularly fungi) for the protection of a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables. [0212] Where a contemplated compound is a fungicide, the compound may be used in crop protection for control of phytopathogenic fungi. A contemplated compound may exhibit outstanding efficacy against a broad spectrum of phytopathogenic fungi, including soil borne pathogens, which are in particular members of the classes Plasmodiophoromycetes, Peronosporomycetes (Syn. Oomycetes), Chytridiomycetes, Zygomycetes, Ascomycetes, Basidiomycetes, and Deuteromycetes (Syn. Fungi imperfecti). Some fungicides are systemically active and may be used in plant protection as foliar, seed dressing or soil fungicide. Furthermore, they are suitable for combating fungi, which, inter alia, infest wood or roots of plant. [0213] Examples of fungi include: one or more members of the phyla of Ascomycota, Oomycota, Basidiomycota, and the subphylum Mucoromycotina. [0214] The fungi of the division Ascomycota include, for example, subdivision Pezizomycotina and Taphrinomycotina which include Dothideomycetes, Leotiomycetes, Sordariomycetes and Taphrinomycetes classes. [0215] The fungi of the phylum Ascomycota include, for example, subphyla selected from the group consisting of Dothideomycetes, Leotiomycetes, and Sordariomycetes. [0216] The fungi of the division Basidiomycota include, for example, subdivisions Agaricomycotina, Pucciniomycotina, and Ustilaginomycotina. [0217] In some embodiments, the one or more target fungi whose growth is to be controlled or inhibited is selected from one or more of the group consisting of Alternaria, Aspergillus, Bipolaris, Blumeria, Botrytis, Candida, Cercospora, Cercosporidium, Claviceps, Cochliobolus, Colletotrichum, Corynespora, Dybotryon, Dilophospora, Erysiphe, Exserohilum, Fusarium, Leveillula, Magnaporthe, Melampsora, Microsphaera, Microsphaeropsis, Monilia, Monilinia, Mycosphaerella, Oidiopsis, Peronospora, Phaeosphaeria, Phakopsora, Phomopsis, Phymatotrichum, Phytophthora, Plasmopora, Podosphaera, Pseudoperonospora, Puccinia, Pyrenophora, Pyricularia, Pythium, Rhizoctonia, Sclerophthora, Sclerotinia, Septoria, Setosphaeria, Uncinula, Ustilago, Venturia, Verticillium, and Zymoseptoria. [0218] Where a contemplated compound is a parasite, the compound may be used as an antiparasiticide in animal health. [0219] Exemplary animal parasites from the phyla Plathelminthes and Nematoda, include, for example, Ancylostoma duodenale, Ancylostoma ceylanicum, Acylostoma braziliensis, Ancylostoma spp., Ascaris spp., Brugia malayi, Brugia timori, Bunostomum spp., Chabertia spp., Clonorchis spp., Cooperia spp., Dicrocoelium spp., Dictyocaulus filaria, Diphyllobothrium latum, Dracunculus medinensis, Echinococcus granulosus, Echinococcus multilocularis, Enterobius vermicularis, Faciola spp., Haemonchus spp., Heterakis spp., Hymenolepis nana, Hyostrongulus spp., Loa Loa, Nematodirus spp., Oesophagostomum spp., Opisthorchis spp., Onchocerca volvulus, Ostertagia spp., Paragonimus spp., Schistosomen spp., Strongyloides fuelleborni, Strongyloides stercoralis, Stronyloides spp., Taenia saginata, Taenia solium, Trichinella spiralis, Trichinella nativa, Trichinella britovi, Trichinella nelsoni, Trichinella pseudopsiralis, Trichostrongulus spp., Trichuris trichiura, and Wuchereria bancrofti. [0220] Where a contemplated compound is a parasite, the compound may be used as in crop protection for control of phytopathogenic nematodes. Such a compound may include an outstanding efficacy against a broad spectrum of phytopathogenic nematodes, including soil borne plant parasitic nematodes. [0221] A contemplated compound may be active against a wide spectrum of nematodes; there are 16 to 20 different orders within the phylum Nematoda. Ten of these orders regularly occur in soil, including four orders, including Rhabditida, Tylenchida, Aphelenchida, and Dorylaimid. Further, plant parasites include many members of the order Tylenchida, and a few genera in the orders Aphelenchida and Dorylaimida. [0222] Phytoparasitic pests from the phylum Nematoda, for example, Aphelenchoides spp., Bursaphelenchus spp., Ditylenchus spp., Globodera spp., Heterodera spp., Longidorus spp., Meloidogyne spp., Pratylenchus spp., Radopholus spp., Trichodorus spp., Tylenchulus spp., Xiphinema spp., Helicotylenchus spp., Tylenchorhynchus spp., Scutellonema spp., Paratrichodorus spp., Meloinema spp., Paraphelenchus spp., Aglenchus spp., Belonolaimus spp., Nacobbus spp., Rotylenchulus spp., Rotylenchus spp., Neotylenchus spp., Dolichodorus spp., Hoplolaimus spp., Punctodera spp., Criconemella spp., Quinisulcius spp., Hemicycliophora spp., Anguina spp., Subanguina spp., Hemicriconemoides spp., Psilenchus spp., Pseudohalenchus spp., Criconemoides spp., Cacopaurus spp., Hirschmaniella spp, and Tetylenchus spp.. [0223] In one aspect of the disclosure, a contemplated compound exhibits efficacy against plant-parasitic nematodes selected from the group consisting of: root-knot nematodes (abbreviated herein as RKN, Meloidogyne spp.), soybean cyst nematodes (abbreviated herein as SCN, Heterodera glycines), cyst nematodes (Heterodera spp.), reniform nematodes (Rotylenchulus reniformis), sting nematodes (Belonolaimus spp.), lance nematodes (Hoplolaimus spp.), and lesion nematodes (Pratylenchus spp.). [0224] Some of the contemplated compounds are systemically active and may be used in plant protection as a foliar nematicide, a seed dressing or a soil-applied nematicide. Furthermore, they are suitable for combating nematodes that infest roots, seed gall, seeds, stems, and/or foliar parts of plants. [0225] Chemical treatment with a compound of the disclosure is the main method for controlling plant-parasitic nematodes. Application methods include fumigation, in furrow, seed treatment, pre- and post planting application through irrigation systems, granules, and broadcast sprays, and bare root dipping/drenching in the case of transplanted seedlings. [0226] In another aspect, the disclosure includes compounds and methods for reducing, ameliorating, or inhibiting an infestation a pest from the phylum Arthropoda, and particularly of its classes Insecta and Arachnida. In some embodiments the insect or arachnid is an ectoparasite. Examples of ectoparasites that infest non-human animals, without being limiting, are arthropod ectoparasites such as biting flies, blow flies, fleas, lice, other sucking insects or dipterous pests, and arachnid members such as ticks and mites. Examples [0227] Section I: Experimental Procedures for Syntheses of Exemplary Compounds [0228] Variables used in general synthetic descriptions may not align with the variables assigned in the claim section. [0229] Example 1: General Procedure for the Preparation of Acyl Diazaborines from 2-Formyl phenyl boronic acids [0230] A suspension of 2-formyl phenyl boronic acid (2.9 mmol, 1 equiv) and benzhydrazide (2.9 mmol, 1 equiv) in EtOH (5 mL) and H ₂ O (5 mL) was stirred at room temperature overnight (about 18 hours). The formed solid was filtered and washed with EtOH, then dried in vacuum to give the desired product as a white solid. [0231] Example 2: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)- yl)(phenyl)methanone [0232] This substance was prepared using the General Procedure. Yield: 33%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.27 (s, 1H), 7.79-7.73 (m, 1H), 7.72-7.64 (m, 3H), 7.63-7.52 (m, 3H), 7.50-7.46 (m, 2H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H12BN ₂ O2251.1, found 251.0. [0233] Example 3: (2-chlorophenyl)(1-hydroxybenzo[d]-[1,2,3]diazaborinin-2(1H) - yl)methanone [0234] This substance was prepared using the General Procedure. Yield: 40%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.11 (s, 1H), 7.87 (d, J = 7.2 Hz, 1H), 7.59-7.47 (m, 7H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H10BClN2O2285.1, found 285.0. [0235] Example 4: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(2- methoxyphenyl)methanone [0236] This substance was prepared using the General Procedure. Yield: 62%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.05 (s, 1H), 7.74 (d, J = 6.8 Hz, 1H), 7.57-7.48 (m, 4H), 7.23 (d, J = 7.6 Hz, 1H), 7.12 (d, J = 7.6 Hz, 1H), 7.03 (dd, J1 = 7.6 Hz, J2 = 7.6 Hz, 1H), 3.72 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₃ BN ₂ O ₃ 281.1, found 281.1. [0237] Example 5: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(4- methoxyphenyl)methanone [0238] This substance was prepared using the General Procedure. Yield: 55%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.28 (s, 1H), 7.73-7.64 (m, 4H), 7.55-7.53 (m, ₂ H), 7.0 (d, J = 8.8 Hz, 2H), 3.81 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C15H13BN ₂ O3281.1, found 281.0. [0239] Example 6: (7-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)- yl)(phenyl)methanone [0240] To a solution of 2-bromo-4-chloro-benzaldehyde (2.18 g, 10 mmol) in ethanol (15 mL) and triethyl orthoformate (2.23 g, 15 mmol) was added a drop of conc. H2SO4 at room temperature, then the reaction mixture was heated to reflux for 1 hour. Water (25 mL) was added to the mixture when HPLC indicated the reaction was complete. The resulting solution was extracted with EtOAc (1 × 25 mL), the extracts were washed by sat. NaHCO3 and brine, then dried over anhydrous Na2SO4, and concentrated in vacuo, giving crude 2-bromo-4-chloro- 1-(diethoxymethyl)benzene (2.1 g, 71%) as yellow oil. This oil was used in the next step without further purification. ¹ H NMR (400 MHz, DMSO-d6) δ7.75 (d, J = 2.0 Hz, 1H), 7.58-7.54 (m, 1H), 7.50 (dd, J1 = 8.4, J2 = 2.0 Hz, 1H), 5.54 (s, 1H), 3.64-3.47 (m, 4H), 1.14 (t, J = 7.0 Hz, 6H) ppm. [0241] A solution of crude 2-bromo-4-chloro-1-(diethoxymethyl)benzene (1.3 g, 4.4 mmol) in dry THF (10 mL) was cooled to -78°C then n-butyl lithium (2.8 mL, 6.6 mmol, 2.4 M in THF) was added dropwise. When the addition was completed, the reaction mixture was allowed to warm to -40 °C over 15 minutes with stirring, then cooled to -78°C again. Isopropyl borate (1.24 g, 6.6 mmol) in THF (2 mL) was added to the reaction slowly, then the reaction mixture was allowed to warm to 0°C and was quenched with 2 M HCl (10 mL). The resulting mixture was stirred at room temperature for 1 hour, diluted by EtOAc (2 × 25 mL), washed with brine and H ₂ O, dried over Na2SO4, and concentrated in vacuo to give the crude product. The crude product was subjected to silica gel chromatography (SiO2, 100-200 m, eluting by DCM/MeOH = 30/1 to 10/1), giving (5-chloro-2-formylphenyl)-boronic acid (300 mg, 37%) as a white foam solid. ¹ H NMR (400 MHz, DMSO-d6): δ 10.11 (s, 1H), 8.39 (s, 2H), 7.92-7.88 (m, 1H), 7.65-7.57 (m, ₂ H) ppm. [0242] (7-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)- yl)(phenyl)methanone: This substance was prepared starting with (5-chloro-2- formylphenyl)boronic acid and benzohydrazide using the General Procedure. Yield: 22%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.31 (s, 1H), 7.74-7.67 (m, 4H), 7.65-7.57 (m, ₂ H), 7.48 (t, J = 7.7 Hz, ₂ H) ppm. [0243] Example 7: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(pyridin-4- yl)methanone [0244] This substance was prepared using the General Procedure. Yield: 32%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.73 (d, J = 6 Hz, 2H), 8.24 (s, 1H), 7.80-7.73 (m, 1H), 7.70-7.62 (m, 3H), 7.61-7.50 (m, 2H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C13H11BN3O2252.1, found 252.1. [0245] Example 8: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(o- tolyl)methanone [0246] This substance was prepared using the General Procedure. Yield: 20%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.12 (s, 1H), 7.78 (d, J = 6.8 Hz, 1H), 7.61-7.53 (m, 3H), 7.42-7.40 (m, 1H), 7.32-7.28 (m, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₄ BN ₂ O ₂ 265.1, found 265.1. [0247] Example 9: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(p- tolyl)methanone [0248] This substance was prepared using the General Procedure. Yield: 29%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.28 (s, 1H), 7.74 (d, J = 2.8 Hz, 1H), 7.72 (d, J = 2.8 Hz, 1H), 7.67-7.54 (m, 4H), 7.29 (d, J = 4.8 Hz, ₂ H), 2.35 (s, 3H) ppm. MS (ESI) (m/z): [M-H]- calculated for C ₁₅ H ₁₂ BN ₂ O ₂ 263.1, found 263.0. [0249] Example 10: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(pyridin-3- yl)methanone [0250] This substance was prepared using the General Procedure. Yield: 75%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.90 (d, J = 1.9 Hz, 1H), 8.73 (dd, J1 = 4.8 Hz, J2 = 1.5 Hz, 1H), 8.27 (s, 1H), 8.11 (td, J1 = 8.0 Hz, J2 = 1.8 Hz, 1H), 7.78-7.73 (m, 1H), 7.68-7.64 (m, 1H), 7.59-7.48 (m, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C13H11BN3O2252.1, found 252.1. [0251] Example 11: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(thiophen-2- yl)methanone [0252] This substance was prepared using the General Procedure. Yield: 73%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.39 (s, 1H), 8.21 (dd, J1 = 5.0 Hz, J2 = 1.3 Hz, 1H), 7.88 (dd, J1 = 4.0 Hz, J2 = 1.3 Hz, 1H), 7.72 (td, J1 = 4.5 Hz, J2 = 2.0 Hz, 2H), 7.59-7.55 (m, 2H), 7.17 (dd, J1= 4.9 Hz, J2 = 4.1 Hz, 1H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C1 ₂ H10BN ₂ O2S 257.1, found 257.1. [0253] Example 12: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(5- methylthiophen-2-yl)methanone

[0254] To a solution of 5-methylthiophene-2-carboxylic acid (1.42 g, 10 mmol) in MeOH (25 mL) was added conc.H2SO4 (0.8 mL) dropwise at room temperature; the resulting reaction mixture was heated to reflux overnight (about 18 hours). Then the reaction mixture was cooled to room temperature, 25 mL of water was added, and the mixture was extracted with EtOAc (30 mL). The organic phase was washed with sat. NaHCO3 (30 mL), dried over Na2SO4, and concentrated in vacuo to give the crude methyl 5-methylthiophene-2-carboxylate (910 mg, yield 58%). The crude product was used to the next step without further purification. ¹ H NMRH NMR (400 MHz, DMSO-d6) δ 7.63 (d, J = 3.7 Hz, 1H), 6.96-6.91 (m, 1H), 3.79 (s, 3H), 2.51 (s, 3H) ppm. [0255] To a solution of methyl 5-methylthiophene-2-carboxylate (910 mg, 5.8 mmol) in MeOH (10 mL) was added hydrazine hydrate (1.0 mL, 20.0 mmol) at room temperature; the resulting mixture was heated to reflux overnight(about 18 hours). The reaction mixture was cooled to room temperature when liquid chromatography–mass spectrometry (LCMS) indicated the reaction was complete. The reaction mixture was concentrated in vacuo to give crude product, which was subjected to silica gel chromatography, eluting with DCM/MeOH (30:1 to 10:1) to give 5-methyl-thiophene-2-carbohydrazide (540 mg, yield 59%) as a white solid. ¹ H NMR (400 MHz, DMSO-d6): δ 9.61 (s, 1H), 7.50 (d, J = 3.6 Hz, 1H), 6.82-6.81 (m, 1H), 4.39 (s, 2H), 2.45 (s, 3H) ppm. [0256] (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(5-methylthio phen-2- yl)methanone: this substance was prepared starting with (2-formyl-phenyl)boronic acid and 5- methylthiophene-2-carbohydrazide using the General Procedure. Yield: 40%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.33 (s, 1H), 7.74-7.66 (m, 3H), 7.59-7.52 (m, 2H), 6.91-6.90 (m, 1H), 2.51 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₃ H ₁₂ BN ₂ O ₂ S 271.1, found 271.1. [0257] Example 13: (3-chlorothiophen-2-yl)(1-hydroxybenzo-[d][1,2,3]diazaborini n- 2(1H)-yl)methanone

[0258] Methyl 3-chlorothiophene-2-carboxylate was prepared starting with 3- chlorothiophene-2-carboxylic acid using the same method employed for the preparation of methyl 5-methylthiophene-2-carboxylate. Yield: 73%. ¹ H NMR (400 MHz, DMSO-d ₆ ): δ 8.01 (d, J = 5.3 Hz, 1H), 7.25 (d, J = 5.3 Hz, 1H), 3.83 (s, 3H) ppm. It was used for the next step without further purification. [0259] 3-Chlorothiophene-2-carbohydrazide was prepared starting with methyl 3- chlorothiophene-2-carboxylate using the same method employed for the preparation of 5- methylthiophene-2-carbohydrazide. Yield: 56%. ¹ H NMR (400 MHz, DMSO-d ₆ ): δ 9.40 (s, 1H), 7.81 (d, J = 5.3 Hz, 1H), 7.13 (d, J = 5.3 Hz, 1H), 4.56 (s, 2H) ppm. (3-Chlorothiophen-2-yl)(1- hydroxybenzo[d]-[1,2,3]diazaborinin-2(1H)-yl)methanone: this substance was prepared starting with (2-formylphenyl)boronic acid and 3-chloro-thiophene-2-carbohydrazide using the General Procedure. Yield: 49%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.34 (s, 1H), 8.25 (d, J = 5.4 Hz, 1H), 7.76-7.68 (m, 2H), 7.62-7.52 (m, 2H), 7.20 (d, J = 5.4 Hz, 1H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₂ H ₉ BClN ₂ O ₂ S 291.0, found 291.0. [0260] Example 14: (4-chlorophenyl)(1-hydroxybenzo[d]-[1,2,3]diazaborinin-2(1H) - yl)methanone [0261] This substance was prepared starting with (2-formylphenyl)boronic acid and 4- chloro-benzhydrazide using the General Procedure. Yield: 65%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.28 (s, 1H), 7.75-7.73 (m, 3H), 7.65 (d, J = 2.4 Hz, 1H), 7.56-7.54 (m, 4H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₄ H ₁₁ BClN ₂ O ₂ 285.1, found 285.0. [0262] Example 15: (6-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)- yl)(phenyl)methanone [0263] This substance was prepared using the General Procedure. Yield: 83%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.29 (s, 1H), 7.80 (d, J = 2.0 Hz, 1H), 7.74 (d, J = 7.9 Hz, 1H), 7.71-7.66 (m, ₂ H), 7.64-7.57 (m, ₂ H), 7.52-7.44 (m, ₂ H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₄ H ₁₁ BClN ₂ O ₂ 285.1, found 285.1. [0264] Example 16: (5-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)- yl)(phenyl)methanone [0265] This substance was prepared using the General Procedure. Yield: 26%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.57 (s, 1H), 7.76-7.68 (m, 3H), 7.66-7.55 (m, 3H), 7.54-7.44 (m, ₂ H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₄ H ₁₁ BClN ₂ O ₂ 285.0, found 285.1. [0266] Example 17: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)- yl)(4(methylthio)phenyl)methanone [0267] This substance was prepared using the General Procedure. Yield: 85%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.29 (s, 1H), 7.76-7.70 (m, 1H), 7.68-7.62 (m, 3H), 7.59-7.51 (m, ₂ H), 7.37-7.28 (m, 2H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₄ BN ₂ O ₂ S 297.1, found 297.1. [0268] Example 18: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(2 (trifluoromethoxy)phenyl) methanone [0269] This substance was prepared using the General Procedure. Yield: 54%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.14 (s, 1H), 7.77-7.69 (m, ₂ H), 7.65-7.57 (m, 3H), 7.57-7.50 (m, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₁ BF ₃ N ₂ O ₃ 335.1, found 335.0. [0270] Example 19: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(4- (trifluoromethoxy)phenyl) methanone [0271] This substance was prepared using the General Procedure. Yield: 64%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.28 (s, 1H), 7.90-7.84 (m, ₂ H), 7.78-7.73 (m, 1H), 7.69-7.66 (m, 1H), 7.59-7.53 (m, 2H), 7.52-7.42 (m, ₂ H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₁ BF ₃ N ₂ O ₃ 335.1, found 335.0. [0272] Example 20: (5-chlorothiophen-2-yl)(1-hydroxybenzo-[d][1,2,3]diazaborini n- 2(1H)-yl)methanone [0273] This substance was prepared using the General Procedure. Yield: 27%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.40 (s, 1H), 7.77-7.69 (m, 3H), 7.62-7.54 (m, ₂ H), 7.21 (d, J = 4.4 Hz, 1H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₂ H ₉ BClN ₂ O ₂ S 291.0, found 291.0. [0274] Example 21: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(4- methylthiazol-2-yl) methanone [0275] This substance was prepared using the General Procedure. Yield: 84%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.49 (s, 1H), 7.99 (s, 1H), 7.81-7.73 (m, ₂ H), 7.61 (dd, J = 5.5, 3.2 Hz, 2H), 2.39 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₂ H ₁₁ BN ₃ O ₂ S 272.1, found 272.0. [0276] Example 22: (3-chlorophenyl)(1-hydroxybenzo[d]-[1,2,3]diazaborinin-2(1H) - yl)methanone [0277] This substance was prepared using the General Procedure. Yield: 45%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.27 (s, 1H), 7.82-7.77 (m, 1H), 7.76-7.71 (m, 1H), 7.68-7.45 (m, 3H), 7.46-7.33 (m, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₄ H ₁₁ BClN ₂ O ₂ 285.1, found 285.1. [0278] Example 23: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(3- (methylthio)phenyl) methanone [0279] 3-(Methylthio)benzohydrazide: to a solution of methyl 3-(methylthio)benzoate (1.3 g, 7.1 mmol) in MeOH (10 mL) was added hydrazine hydrate (1.0 mL, 20.0 mmol) at room temperature. The resulting mixture was heated to reflux overnight (about 18 hours). The reaction mixture was cooled to room temperature when LCMS indicated the reaction was complete, then concentrated in vacuo to give a residue. The residue was subjected to silica gel chromatography (DCM/MeOH (30:1 to 10:1) to give 3-(methylthio)benzohydrazide (1.1 g, yield 85%) as a white solid. ¹ H NMR (400 MHz, DMSO-d6): δ 9.82 (s, 1H), 7.67 (s, 1H), 7.58 (d, J = 3.4 Hz, 1H), 7.39 (dd, J = 3.8, 2.0 Hz, ₂ H), 4.35 (s, ₂ H), 2.52 (s, 3H). [0280] (1-Hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(3-(methylthi o)phenyl) methanone: this substance was prepared starting with (2-formyl-phenyl)boronic acid and 3- (methylthio)benzohydrazide using the General Procedure. Yield: 45%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.27 (s, 1H), 7.74 (dd, J1 = 5.8 Hz, J2 = 2.6 Hz, 1H), 7.65 (dt, J1 = 7.2 Hz, J2 = 3.1 Hz, 1H), 7.59-7.52 (m, 3H), 7.51-7.46 (m, 1H), 7.43-7.38 (m, 2H), 2.48 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C15H14BN ₂ O2S 297.0, found 297.0. [0281] Example 24: (4-chlorothiophen-2-yl)(1-hydroxybenzo-[d][1,2,3]diazaborini n- 2(1H)-yl) methanone [0282] 4-Chlorothiophene-2-carbohydrazide was prepared starting with methyl 4- chlorothiophene-2-carboxylate using the same method employed for the preparation of 5- methylthiophene-2-carbohydrazide (Example 12). Yield: 64%. ¹ H NMR (400 MHz, DMSO-d6): δ 9.409.87 (s, 1H), 7.81 (d, J = 1.3 Hz, 1H), 7.69 (d, J = 1.4 Hz, 1H), 4.52 (s, ₂ H) ppm. [0283] (4-Chlorothiophen-2-yl)(1-hydroxybenzo-[d][1,2,3]diazaborini n-2(1H)-yl) methanone: this substance was prepared starting with (2-formyl-phenyl)boronic acid and 4- chlorothiophene-2-carbohydrazide using the General Procedure. Yield: 27%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.41 (s, 1H), 8.23 (d, J = 1.6 Hz, 1H), 7.83-7.63 (m, 3H), 7.63-7.49 (m, ₂ H) ppm. MS (ESI) (m/z): [M-H]- calculated for C1 ₂ H7BClN ₂ O2S 289.0, found 288.9. [0284] Example 25: (2,6-dimethylphenyl)(1-hydroxybenzo-[d][1,2,3]diazaborinin- 2(1H)-yl) methanone [0285] This substance was prepared using the General Procedure. Yield: 52%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.10 (s, 1H), 7.74 (m, 1H), 7.60-7.52 (m, 3H), 7.27 (dd, J ₁ =J ₂ = 7.6 Hz 1H), 7.13 (d, J = 7.6 Hz, 1H), 7.08 (d, J = 7.6 Hz, 1H), 2.25 (s, 3H), 2.05 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₆ H ₁₆ BN ₂ O ₂ 279.1, found 279.1. [0286] Example 26: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(6- methylpyridin-3-yl)methanone [0287] This substance was prepared using the General Procedure. Yield: 25%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.27 (s, 1H), 7.76-7.53 (m, 8H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₁ BF ₃ N ₂ O ₃ 335.0, found 335.0. [0288] Example 27: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(4- methylthiophen-2-yl)methanone [0289] This substance was prepared using the General Procedure. Yield: 25%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.37 (s, 1H), 7.83 (s, 1H), 7.76-7.64 (m, 3H), 7.60-.52 (m, ₂ H), 2.17 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C13H12BN ₂ O2S 271.1, found 271.0. [0290] Example 28: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(5- methylthiazol-2-yl)methanone [0291] This substance was prepared using the General Procedure. Yield: 55%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.46 (s, 1H), 7.86 (d, J = 0.8 Hz, 1H), 7.80-7.75 (m, 1H), 7.75-7.71 (m, 1H), 7.64-7.54 (m, 2H), 2.56 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₂ H ₁₁ BN ₃ O ₂ S 272.1, found 272.0. [0292] Example 29: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(pyridin-2- yl)methanone [0293] This substance was prepared using the General Procedure. Yield: 25%. ¹ H NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 5.4 Hz, 1H), 8.55 (dd, J1 = 7.8 Hz, J2 = 1.0 Hz, 1H), 8.22 (d, J = 7.8 Hz, 1H), 8.17-8.10 (m, 1H), 8.06 (s, 1H), 7.82 (d, J = 6.9 Hz, 1H), 7.50 (d, J = 7.6 Hz, 1H), 7.42-7.37 (m, 2H), 4.13 (s, 1H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C13H11BN3O2 252.1, found 252.1. HPLC purity: 97.72% purity at 210 nm and 97.94% purity at 254 nm. [0294] Example 30: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(6- methylpyridin-2-yl) methanone OH O [0295] This substance was prepared using the General Procedure. Yield: 27%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.41 (t, J = 7.8 Hz, 1H), 8.11 (s, 1H), 8.03 (d, J = 7.4 Hz, 1H), 7.98 (d, J = 7.9 Hz, 1H), 7.70-7.63 (m, 1H), 7.52 (dd, J1 = 6.1 Hz, J2 = 2.7 Hz, 1H), 7.40 (dd, J1 = 6.1 Hz, J2 = 2.5 Hz, ₂ H), 4.20 (s, 1H), 3.21 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H13BN3O2266.1, found 266.1. HPLC purity: 98.61% purity at 210 nm and 97.86% purity at 254 nm. [0296] Example 31: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(1-methyl-1H- benzo[d]imidazole-2-yl) methanone [0297] This substance was prepared using the General Procedure. Yield: 25%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.14 (d, J = 8.0 Hz, 1H), 8.02 (d, J = 3.8 Hz, 1H), 8.01 (d, J = 3.8 Hz, 1H), 7.77 (d, J = 6.9 Hz, 1H), 7.70-7.65 (m, ₂ H), 7.49 (d, J = 7.3 Hz, 1H), 7.45-7.37 (m, 2H), 4.24 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C16H14BN4O2305.1, found 305.0. [0298] Example 32: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(m- tolyl)methanone [0299] This substance was prepared using the General Procedure. Yield: 18%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.27 (s, 1H), 7.74 (d, J = 5.9 Hz, 1H), 7.68-7.63 (m, 1H), 7.59-7.52 (m, 2H), 7.46-7.45 (m, 2H), 7.42-7.34 (m, 2H), 2.31 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₄ BN ₂ O ₂ 265.1, found 265.1. [0300] Example 33: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(3- methylthiophen-2-yl)methanone [0301] This substance was prepared using the General Procedure. Yield: 64%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.32 (s, 1H), 8.08 (d, J = 5.1 Hz, 1H), 7.81-7.62 (m, 2H), 7.61-7.47 (m, 2H), 7.02 (d, J = 5.1 Hz, 1H), 2.09 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₃ H ₁₂ BN ₂ O ₂ S 271.1, found 271.1. [0302] Example 34: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(thiazol-2- yl)methanone [0303] This substance was prepared using the General Procedure. Yield: 38%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.50 (s, 1H), 8.38 (d, J = 3.0 Hz, 1H), 8.12 (d, J = 3.0 Hz, 1H), 7.81-7.71 (m, 2H), 7.65-7.57 (m, ₂ H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₁ H ₉ BN ₃ O ₂ S 258.1, found 258.0. [0304] Example 35: 1-(1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)ethan-1-one [0305] This substance was prepared using the General Procedure. Yield: 68%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.14 (s, 1H), 7.64-7.58 (m, ₂ H), 7.5-7.91 (m, 2H), 2.39 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₉ H ₁₀ BN ₂ O ₂ 189.1, found 189.0. [0306] Example 36: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(2- (methylthio)phenyl)methanone [0307] This substance was prepared using the General Procedure. Yield: 40%. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.07 (s, 1H), 7.77 (d, J = 7.1 Hz, 1H), 7.61-7.46 (m, 5H), 7.34 (dd, J = 12.7, 7.1 Hz, 2H), 2.42 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₃ BN ₂ O ₂ S 297.1, found 297.1. [0308] Example 37: N-(4-(1-hydroxy-1,2-dihydrobenzo[d]-[1,2,3]diazaborinine-2- carbonyl)phenyl) methanesulfonamide [0309] N-(4-(Hydrazinecarbonyl)phenyl)-methanesulfonamide was prepared starting with ethyl 4-(methylsulfonamido)benzoate using the same method employed for the preparation of 5-methylthiophene-2-carbohydrazide (Example 12). Yield: 75%. ¹ H NMR (400 MHz, DMSO- d6): δ 9.63 (s, 1H), 7.77 (d, J = 8.6 Hz, 2H), 7.18 (d, J = 8.6 Hz, ₂ H), 4.43 (s, 2H), 3.02 (s, 3H) ppm. [0310] N-(4-(1-Hydroxy-1,2-dihydrobenzo[d][1,2,3]-diazaborinine-2- carbonyl)phenyl) methanesulfonamide: this substance was prepared starting N-(4- (hydrazine-carbonyl)phenyl)methanesulfonamide and 2-formyl-phenylboronic acid using the General Procedure. Yield: 15.7 %. ¹ H NMR (400 MHz, DMSO-d6) δ 10.35 (s, 1H), 8.28 (s, 1H), 7.74 -7.61 (m, 4H), 7.61-7.45 (m, 2H), 7.24 (d, J = 8.8 Hz, ₂ H), 3.08 (s, 3H) ppm. MS (ESI) (m/z): [M-H]- calculated for C15H13BN3O4S 342.1, found 342.0. [0311] Example 38: 4-(1-hydroxy-1,2-dihydrobenzo[d][1,2,3]-diazaborinine-2- carbonyl) benzenesulfonamide [0312] This substance was prepared using the General Procedure. Yield: 8.4 %. ¹ H NMR (400 MHz, DMSO-d ₆ ) δ 8.27 (s, 1H), 7.93-7.84 (m, 4H), 7.79-7.74 (m, 1H), 7.69-7.64 (m, 1H), 7.60-7.51 (m, 4H) ppm. MS (ESI) (m/z): [M-H]- calculated for C ₁₄ H ₁₁ BN ₃ O ₄ S 328.1, found 328.0. [0313] Example 39: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(6- methylpyridin-3-yl) methanone [0314] This substance was prepared using the General Procedure. Yield: 85%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.78 (d, J = 1.8 Hz, 1H), 8.27 (s, 1H), 8.00-7.97 (m, 1H), 7.75-7.55 (m, 4H), 7.37 (d, J = 8.2 Hz, 1H), 2.52 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₄ H ₁₃ BN ₃ O ₂ 266.1, found 266.1. [0315] Example 40: 3-(1-hydroxy-1,2-dihydrobenzo[d][1,2,3]-diazaborinine-2- carbonyl) benzenesulfonamide [0316] This substance was prepared using the General Procedure. Yield: 26.3%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.28 (s, 1H), 8.10 (s, 1H), 8.01 (d, J = 7.5 Hz, 1H), 7.95 (d, J = 7.8 Hz, 1H), 7.76-7.66 (m, 3H), 7.57-7.55 (m, ₂ H), 7.47 (s, 2H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H13BN3O4S 330.1, found 330.1. [0317] Example 41: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(3- (methylsulfonyl)phenyl) methanone [0318] This substance was prepared using the General Procedure. Yield: 19%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.29 (s, 1H), 8.25 (s, 1H), 8.14 (d, J = 7.9 Hz, 1H), 8.05 (d, J = 8.0 Hz, 1H), 7.78-7.72 (m, ₂ H), 7.70-7.63 (m, 1H), 7.61-7.51 (m, ₂ H), 3.25 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₄ BN ₂ O ₄ S 329.1, found 329.0. [0319] Example 42: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(3- methoxyphenyl) methanone [0320] This substance was prepared using the General Procedure. Yield: 8%. ¹ H NMR (400 MHz, DMSO-d6) δ 8.26 (s, 1H), 7.74 (d, J = 5.2 Hz, 1H), 7.65 (s, 1H), 7.55 (s, 2H), 7.39 (dd, J1 = J2 = 7.6 Hz, 1H), 7.30-7.13 (m, 3H), 3.76 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C15H14BN ₂ O3281.1, found 281.1. [0321] Example 43: N-(3-(1-hydroxy-1,2-dihydrobenzo[d]-[1,2,3]diazaborinine-2- carbonyl)phenyl) methanesulfonamide O O [0322] To a solution of ethyl 3-(methylsulfon-amido)benzoate (500 mg, 2.06 mmol) in EtOH (5 mL) was added hydrazine hydrate (0.8 mL, 16.0 mmol) at room temperature. This mixture was heated to reflux overnight (about 18 hours). The reaction mixture was cooled to room temperature when LCMS indicated the reaction was complete. The mixture was concentrated in vacuo to give a residue that was subjected to silica gel chromatography (DCM/MeOH (30:1 to 10:1)) to give N-(3-(hydrazinecarbonyl)phenyl) methanesulfonamide (400 mg, yield 87%) as a white solid. ¹ H NMR (400 MHz, DMSO-d ₆ ): δ 9.55 (s, ₂ H), 7.56 (s, 1H), 7.39 (d, J = 7.5 Hz, 1H), 7.32 (t, J = 7.7 Hz, 1H), 7.26 (d, J = 7.9 Hz, 1H), 4.35 (s, 2H), 2.94 (s, 3H) ppm. [0323] A suspension of (2-formylphenyl)boronic acid (450 mg, 3 mmol) and N-(3- (hydrazinecarbonyl)-phenyl) methanesulfonamide in i-PrOH (5 mL) was stirred at room temperature overnight (18 hours). The resulting precipitate was filtered, washed with i-PrOH (2 mL), and then dried in vacuo to give N-(3-(1-hydroxy-1,2- dihydrobenzo[d][1,2,3]diazaborinine-2-carbonyl)-phenyl) methanesulfonamide (29 mg, 5.2%) as a white solid. ¹ H NMR (400 MHz, DMSO-d6): δ 9.94 (br, 1H), 8.28 (s, 1H), 7.78-7.70 (m, 1H), 7.67 (dd, J1 = 6.8 Hz, J2 = 1.9 Hz, 1H), 7.60-7.51 (m, ₂ H), 7.51 (d, J = 1.1 Hz, 1H), 7.44 (d, J = 5.5 Hz, ₂ H), 7.40 (dd, J1 = 4.3 Hz, J2 = 1.7 Hz, 1H), 2.99 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C15H15BN3O4S 344.1, found 344.1. [0324] Example 44: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(4- (methylsulfonyl)phenyl) methanone [0325] This substance was prepared using the General Procedure. Yield: 21 %. ¹ H NMR (400 MHz, DMSO-d6) δ 8.25 (s, 1H), 8.02 (d, J = 8.6 Hz, ₂ H), 7.96 (d, J = 8.6 Hz, ₂ H), 7.77-7.73 (m, 1H), 7.68-7.64 (m, 1H), 7.60-7.52 (m, 2H), 3.32 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C15H14BN ₂ O4S 329.1, found 329.1. [0326] Example 45: (8-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)- yl)(phenyl)methanone [0327] To a solution of 2-bromo-3-chloro-benzaldehyde (2.2 g, 10 mmol) in dioxane (30 mL) was added bis(pinacolato)diboron (5.1 g, 20 mmol), 1,1′- bis(diphenylphosphino)ferrocene]dichloropalladium(II) [Pd(dppf)Cl ₂ ] (820 mg, 1 mmol) and AcOK (2.96 g, 30 mmol) at room temperature under N ₂ atmosphere. The resulting mixture was heated to 80 ℃ for 2 hours. The reaction mixture was cooled to room temperature when TLC (PE/EA=10:1) indicated the reaction was complete. The mixture was diluted with EtOAc (20 mL), washed with water and concentrated in vacuo, giving a residue that was subjected to silica gel chromatography (PE/EtOAc: from100:1 to 30:1) to give 3-chloro-2-(4,4,5,5-tetramethyl- 1,3,2-dioxaborolan-2-yl)benzaldehyde (2.1 g, yield 78%) as a white solid. ¹ H NMR (400 MHz, CDCl ₃ ): δ 9.86 (s, 1H), 7.62 (dd, J1 = 7.5 Hz, J2 = 1.0 Hz, 1H), 7.50 (dd, J1 = 8.0 Hz, J2 = 1.0 Hz, 1H), 7.41 (d, J = 7.5 Hz, 1H), 1.41 (s, 12H) ppm. [0328] To a suspension of 3-chloro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (530 mg, 2 mmol) in THF and H ₂ O (v/v=1/1, 3 mL) was added NaIO4 (640 mg, 3 mmol, in portions) and AcONH4 (300 mg, 4 mmol). The resulting mixture was stirred at room temperature overnight (about 18 hours). The reaction mixture was filtered, and the filtrate was concentrated in vacuo to yield a crude (2-chloro-6-formylphenyl)boronic acid, which was used in the next step without any further purification (400 mg, crude). ¹ H NMR (400 MHz, DMSO-d6): δ 10.00 (s, 1H), 8.20 (s, ₂ H), 7.93 (d, J = 7.4 Hz, 1H), 7.73 (d, J = 7.9 Hz, 1H), 7.62 (d, J = 7.7 Hz, 1H) ppm. [0329] (2-Chloro-6-formylphenyl)boronic acid (400 mg, 2 mmol) and benzohydrazide (230 mg, 1.7 mmol) was dissolved in i-PrOH (2 mL). The resulting mixture was stirred at room temperature overnight (about 18 hours), the mixture was filtered, and the filter cake was collected and dried by lyophilization to give (8-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin- 2(1H)-yl)(phenyl)methanone (75 mg. yield 15.6%) as a white powder. ¹ H NMR (400 MHz, DMSO-d6): δ 8.14 (s, 1H), 7.86 (d, J = 7.3 Hz, ₂ H), 7.57 (m, 6H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H11BClN ₂ O2285.1, found 285.0. [0330] Example 46: (E)-(2-((2-(2-methylisonicotinoyl)- hydrazineylidene)methyl)phenyl)boronic acid [0331] A suspension of (2-formylphenyl)boronic acid (450 mg, 3 mmol) and 2- methylisonicotino-hydrazide (302 mg, 2 mmol) in i-PrOH (5 mL) was stirred at room temperature overnight. The resulting precipitate was filtered, washed with EtOH (2 mL), and then dried in vacuo to give (E)-(2-((2-(2-methylisonicotinoyl)hydrazineylidene) methyl)-phenyl)boronic acid (127 mg, 22%) as a white solid. ¹ H NMR (400 MHz, DMSO-d6) δ 12.11 (s, 1H), 8.80 (s, 1H), 8.63 (d, J = 5.1 Hz, 1H), 8.49 (s, 2H), 7.96 (d, J = 7.4 Hz, 1H), 7.71 (s, 1H), 7.63 (dd, J ₁ =J ₂ = 5.1 Hz, 2H), 7.48-7.33 (m, ₂ H), 2.58 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H15BN3O3284.1, found 284.1. [0332] Example 47: (E)-(2-((2-(4-acetamidophenyl)- hydrazineylidene)methyl)phenyl)boronic acid [0333] This substance was prepared using a similar procedure as that for (E)-(2-((2-(2- methyl-isonicotinoyl)hydrazineylidene)methyl)phenyl)boronic acid. ¹ H NMR (400 MHz, DMSO- d6) δ δ11.85 (s, 1H), 10.21 (s, 1H), 8.89 (s, 1H), 8.50 (s, ₂ H), 7.97-7.81 (m, 3H), 7.70 (d, J = 8.6 Hz, 2H), 7.62 (d, J = 7.2 Hz, 1H), 7.48-7.34 (m, ₂ H), 2.08 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C16H17BN3O4326.1, found 326.1. [0334] Example 48: (E)-(2-((2-(oxazole-2-carbonyl)- hydrazineylidene)methyl)phenyl)boronic acid [0335] This substance was prepared using a similar procedure as that for (E)-(2-((2-(2- methyl-isonicotinoyl)hydrazineylidene)methyl)phenyl)boronic acid. Yield: 22%. ¹ H NMR (400 MHz, DMSO-d6) δ 12.54 (s, 1H), 8.89 (s, 1H), 8.42 (s, 1H), 8.40 (s, ₂ H), 7.91 (d, J1 = 7.2 Hz, 1H), 7.61-7.59 (m, 1H), 7.54 (s, 1H), 7.46-7.38 (m, ₂ H) ppm. MS (ESI) (m/z): [M-H]- calculated for C11H9BN3O4258.1, found 258.1. [0336] Example 49: (E)-(2-((2-(5-methyloxazole-2-carbonyl)- hydrazineylidene)methyl)phenyl) boronic acid [0337] To a solution of methyl 5-methyloxazole-2-carboxylate (500 mg, 3.5 mmol) in EtOH (2 mL) was added hydrazine hydrate (0.5 mL, 10.0 mmol) at room temperature and the resulting mixture was stirred at room temperature for 3 hours. The solid that formed was collected by filtration and dried in vacuo to give 5-methyloxazole-2-carbohydrazide (300 g, yield 60%) as an off-white solid. ¹ H NMR (400 MHz, DMSO-d6): δ 10.03 (s, 1H), 7.03 (d, J = 1.0 Hz, 1H), 4.56 (s, 2H), 2.36 (d, J = 1.0 Hz, 3H) ppm. [0338] (E)-(2-((2-(5-Methyloxazole-2-carbonyl)-hydrazineylidene)met hyl)phenyl) boronic acid: this substance was prepared using the General Procedure. Yield: 50%. ¹ H NMR (400 MHz, DMSO-d6) δ 12.43 (s, 1H), 8.87 (s, 1H), 8.43 (s, 2H), 7.91 (d, J = 7.3 Hz, 1H), 7.61 (dd, J1 = 7.1 Hz, J2 = 1.1 Hz, 1H), 7.49-7.30 (m, ₂ H), 7.16 (d, J = 1.0 Hz, 1H), 2.43 (d, J = 1.0 Hz, 3H) ppm. MS (ESI) (m/z): [M-H]- calculated for C1 ₂ H11BN3O4272.1, found 272.1. [0339] Example 50: (6-chloro-1-hydroxy-2,3,1-benzodiaza-borinin-2-yl)-(2- fluorophenyl) methanone [0340] To a solution of 2-fluorobenzohydrazide (100 mg, 650.81 µmol, 1.2 eq) and (4- chloro-2-formyl-phenyl)boronic acid (0.1 g, 542.34 µmol, 1 eq) in EtOH (3 mL) was added NH3- H ₂ O (380 mg, 2.71 mmol, 417.78 µL, 25% purity, 5 eq). The resulting mixture was stirred at 60°C for 2 hours. The reaction mixture was concentrated in vacuo to give a residue that was purified by prep-HPLC (column: Xtimate® C18150*25mm*5 µm (Welsh Materials, Inc.; Shanghai, China); mobile phase: [water (0.04% NH3H ₂ O + 10 mM NH ₄ HCO ₃ )-ACN]; B%: 10%- 40%, 10.5 minutes) to give (6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)- (2-fluorophenyl)methanone (95 mg, 56% yield) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.22 (s, 1H), 7.78-7.76 (m, ₂ H), 7.67-7.60 (m, ₂ H), 7.60-7.50 (m, 1H), 7.36-7.32 (m, ₂ H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H10BClFN ₂ O2303.0, found 303.1. HPLC purity: 97.33% (220 nm), 95.28% (254 nm). [0341] Example 51: (6-chloro-1-hydroxy-2,3,1-benzo-diazaborinin-2-yl)-(2- chlorophenyl) methanone [0342] This substance was prepared using a similar procedure as that for (6-chloro-1- hydroxy-2,3,1-benzodiazaborinin-2-yl)(2-fluorophenyl)methano ne. Yield: 55%. ¹ H NMR (DMSO- d6, 400 MHz) δ 8.14 (s, 1H), 7.78-7.74 (m, 2H), 7.64-7.47 (m, 5H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C14H10BCl ₂ N ₂ O2319.0, found 319.0. HPLC purity: 98.28% (220 nm), 96.66% (254 nm). [0343] Example 52: (6-chloro-1-hydroxy-2,3,1-benzodiaza-borinin-2-yl)-(4- methoxyphenyl) methanone [0344] This substance was prepared using a similar procedure as that for (6-chloro-1- hydroxy-2,3,1-benzodiazaborinin-2-yl)(2-fluorophenyl)methano ne. Yield: 74%. ¹ H NMR (DMSO- d ₆ , 400 MHz) δ 8.31 (s, 1H), 7.81 (s, 1H), 7.74-7.10 (dd, J ₁ = 2.0 Hz, J ₂ = 8.8 Hz, 3H), 7.58-7.60 (d, J = 8.0 Hz, 1H), 7.03-7.00 (d, J = 8.8 Hz, 2H), 3.82 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₃ BClN ₂ O ₃ 315.1, found 315.1. HPLC purity: 100% (220 nm), 100% (254 nm). [0345] Example 53: (6-chloro-1-hydroxy-2,3,1-benzodiaza-borinin-2-yl)-(2-chloro -4- methoxy-phenyl)methanone [0346] To a solution of 2-chloro-4-methoxy-benzoic acid (431 mg, 2.31 mmol, 1 eq) in DCM (8 mL) was added EDCI (531 mg, 2.77 mmol, 1.2 eq), HOBt (31 mg, 230.82 µmol, 0.1 eq), TEA (700 mg, 6.92 mmol, 963.83 µL, 3 eq) and tert-butyl N-aminocarbamate (336 mg, 2.54 mmol, 1.1 eq). The mixture was stirred at 25°C for 12 hours. Then the reaction mixture was poured into water (10 mL) and extracted with ethyl acetate (10 mL x 3). The combined organic phase was washed with brine (20 mL), dried over anhydrous Na ₂ SO ₄ , and concentrated in vacuo. The resulting residue was purified by silica gel chromatography (Petroleum ether/Ethyl acetate = 100/1, 3/1) to afford tert-butyl N-[(2-chloro-4-methoxy-benzoyl)amino]carbamate (0.45 g, 1.50 mmol, 65% yield) as an off-white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 9.88 (br, 1H), 8.93 (br, 1H), 7.37 (d, 1H), 7.06 (s, 1H), 6.98-6.95 (m, 1H), 3.79 (s, 3H), 1.44-1.36 (m, 9H). [0347] A mixture of tert-butyl N-[(2-chloro-4-methoxy-benzoyl)amino]carbamate (450 mg, 1.50 mmol, 1 eq) and HCl/EtOAc (4 M, 19.3 mL, 51.55 eq) in a bottom flask was stirred at 25°C for 3 hours. The resulting mixture was concentrated in vacuo to give a residue, H ₂ O (10 mL) was added, and the pH value of the resulting mixture was adjusted to 7-8 by adding aq. Na ₂ CO ₃ . The mixture was then extracted with ethyl acetate (10 mL x 3), and the combined organic phase was washed with brine (20 mL), dried over anhydrous Na ₂ SO ₄ , and concentrated in vacuo to give 2-chloro-4-methoxybenzohydrazide (0.2 g, 67% yield) as a white solid. This product was used in the next step directly without further purification. ¹ H NMR (CDCl ₃ , 400 MHz) δ 9.51 (s, 1H), 7.39 (d, J = 8.8 Hz, 1H), 7.12 (d, J = 2.8 Hz, 1H), 7.00 (dd, J1 = 2.8 Hz, J2 = 8.8 Hz, 1H), 4.51 (br. s, 1H), 3.86 (s, 3H). [0348] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (202 mg, 1.10 mmol, 1.1 eq) and 2-chloro-4-methoxy-benzohydrazide (0.2 g, 996.90 µmol, 1 eq) in EtOH (4 mL) was added NH3-H ₂ O (700 mg, 4.98 mmol, 767.94 µL, 25% purity, 5 eq). The mixture was stirred at 60°C for 2 hours, and then concentrated in vacuo to give a residue. To the residue was added CH ₃ CN (5 mL), the resulting mixture was stirred at 25°C for 5 minutes. The formed precipitate was collected by filtration and dried in vacuo to give (6-chloro-1-hydroxy-2,3,1- benzodiazaborinin-2-yl)-(2-chloro-4-methoxy-phenyl)methanone (152 mg, 44% yield) as a white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 8.12 (s, 1H), 7.73 (d, J = 8.0 Hz, 2H), 7.59 (dd, J ₁ = 8.4, J ₂ = 2.4 Hz, 1H), 7.41 (d, J = 8.4 Hz, 1H), 7.13 (d, J = 2.4Hz, 1H), 6.99 (dd, J ₁ = 8.8 Hz, J ₂ = 2.4 Hz, 1H), 3.80 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₅ H ₁₂ BCl ₂ N ₂ O ₃ 349.0, found 349.1. HPLC purity: 100% (220 nm), 100% (254 nm). [0349] Example 54: (6-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)-yl)(2- methoxyphenyl)methanone [0350] This substance was prepared using the same procedure as that for (6-chloro-1- hydroxy-2,3,1-benzodiazaborinin-2-yl)(2-fluorophenyl) methanone. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.10 (s, 1H), 7.76-7.74 (m, ₂ H), 7.61-7.59 (dd, J = 2.0, 8.0 Hz, 1H), 7.61 (t, J = 8.0 Hz, 1H), 7.26 (d, J = 8.0 Hz, 1H), 7.15 (d, J = 8.4 Hz, 1H), 7.04 (t, J = 8.0 Hz, 1H), 3.73 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C15H13BClN ₂ O3315.1, found 315.1. HPLC purity: 94.6% (220 nm), 97.5% (254 nm). [0351] Example 55: (6-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)-yl)(3- chlorothiophen-2-yl)methanone [0352] This substance was prepared using the same procedure as that for (6-chloro-1- hydroxy-2,3,1-benzodiazaborinin-2-yl)(2-fluorophenyl) methanone. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.36 (s, 1H), 8.28 (d, J = 5.2 Hz, 1H), 7.85 (s, 1H), 7.73 (d, J = 8.0 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.23 (d, J = 5.2 Hz, 1H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C1 ₂ H8BCl ₂ N ₂ O2S 325.0, found 325.0. HPLC purity: 100% (220 nm), 100% (254 nm). [0353] Example 56: (6-chloro-1-hydroxy-2,3,1-benzo-diazaborinin-2-yl)-(3-methox y- 2-thienyl)methanone [0354] To a solution of methyl 3-hydroxythiophene-2-carboxylate (0.3 g, 1.90 mmol, 1 eq) in DMF (3 mL) was added Cs2CO3 (1.54 g, 4.74 mmol, 2.5 eq) and MeI (404 mg, 2.84 mmol, 177.11 µL, 1.5 eq). The resulting mixture was stirred at room temperature for 5 hours. The mixture was then poured into ice-H ₂ O (10 mL) and extracted with ethyl acetate (10 mL x 3). The combined organic phase was washed with brine (10 mL), dried over anhydrous Na ₂ SO ₄ , filtered, and concentrated in vacuo. The crude product was purified by silica gel chromatography (Petroleum ether/Ethyl acetate = 100/1, 1/1) to afford methyl 3- methoxythiophene-2-carboxylate (0.2 g, 61% yield) as an off-white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ7.41 (d, J = 5.2 Hz, 1H), 6.86 (d, J = 5.6 Hz, 1H), 3.99 (s, 3H), 3.84 (s, 3H) [0355] To a solution of methyl 3-methoxythiophene-2-carboxylate (0.1 g, 580.72 µmol, 1 eq) in EtOH (5 mL) was added NH ₂ NH ₂ -H ₂ O (233 mg, 1.16 mmol, 225.79 µL, 25% purity, 2 eq). The mixture was stirred at 90°C for 12 hours and then concentrated to give 3-methoxythiophene-2-carbohydrazide (0.1 g, crude) as a brown oil, which was used in the next step directly without further purification. [0356] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (90 mg, 487.79 µmol, 1.2 eq) and 3-methoxythiophene-2-carbohydrazide (70 mg, 406.49 µmol, 1 eq) in EtOH (2 mL) was added K ₂ CO ₃ (140 mg, 1.02 mmol, 2.5 eq). The mixture was stirred at 60°C for 2 hours and then concentrated to give a residue. To the residue was added cold-EtOH (5 mL) and the resulting mixture was stirred at 0°C for 5 minutes. The formed precipitate was collected by filtration and dried in vacuo to give a solid, which was then freeze-dried to give (6-chloro-1- hydroxy-2,3,1-benzodiazaborinin-2-yl)-(3-methoxy-2-thienyl) methanone (91 mg, 70% yield) as a light yellow solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.24 (s, 1H), 8.12 (d, J = 5.6 Hz, 1H), 7.79 (s, 1H), 7.66 (d, J = 7.6 Hz, 1H), 7.56 (d, J = 8.0 Hz, 1H), 7.07 (d, J = 5.6 Hz, 1H), 3.65 (s, 1H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C13H11BClN ₂ O3S 321.0, found 321.1. HPLC purity: 90.9% (220 nm), 73.53% (254 nm). [0357] Example 57: (6-chloro-1-hydroxybenzo[d][1,2,3]-diazaborinin-2(1H)-yl)(5- methylthiazol-2-yl)methanone [0358] To a solution of 5-methylthiazole-2-carboxylic acid (0.3 g, 2.10 mmol, 1 eq) in DCM (6 mL) was added EDCI (482 mg, 2.51 mmol, 1.2 eq), HOBt (28 mg, 209.55 µmol, 0.1 eq) and TEA (636 mg, 6.29 mmol, 875.01 µL, 3 eq). The mixture was stirred at room temperature for 0.5 hour. To the mixture was added tert-butyl N-aminocarbamate (291 mg, 2.20 mmol, 1.05 eq) in one portion and the mixture was stirred at room temperature for 12 hours. After completion, the reaction was quenched with H ₂ O (10 mL). Two batches of reaction were combined and worked up together. The combined mixture was extracted with DCM (15 mL x3), and the combined organic layers was washed with brine (15 mL), dried over Na2SO4, filtered and concentrated in vacuo to give a residue that was purified by silica gel chromatography (Petroleum ether/Ethyl acetate = 100/1 to 1/1) to afford tert-butyl 2-(5-methylthiazole-2- carbonyl)hydrazine-1-carboxylate (0.2 g, 19% yield) as light yellow oil. ¹ H NMR (DMSO-d6, 400 MHz) δ 10.46 (s, 1H), 9.04 (s, 1H), 7.82 (s, 1H), 2.53 (s, 3H), 1.45 (s, 9H). [0359] A solution of tert-butyl N-[(5-methyl-thiazole-2-carbonyl)amino]carbamate (0.2 g, 777.28 µmol, 1 eq) in HCl/EtOAc (4 M, 1 mL) was stirred at 25°C for 2 hours. The mixture was concentrated to give 5-methylthiazole-2-carbohydrazide hydrochloride (0.1 g, crude) as a white solid, which was used in the next step directly without further purification. [0360] To a solution of 5-methylthiazole-2-carbohydrazide hydrochloride (30 mg, 154.92 µmol, 1 eq) in EtOH (3 mL) was added K ₂ CO ₃ (21 mg, 154.92 µmol, 1 eq). The mixture was stirred for 30 minutes at room temperature, then (4-chloro-2-formyl-phenyl)boronic acid (29 mg, 154.92 µmol, 1 eq) was added, and the resulting mixture was stirred at 60°C for 2 hours. The reaction mixture was concentrated in vacuo to give a residue that was purified by prep-HPLC (column: Xamide® 150*30mm 5µm; mobile phase: [water (0.04% NH3H ₂ O+10 mM NH ₄ HCO ₃ )- ACN]; B%: 15%-35%, 10.5 minutes) to give the crude product. The crude product was washed with EtOH (2 mL) and stirred at room temperature for 2 minutes. The formed precipitate was collected and dried in vacuo to give (6-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(5- methylthiazol-2-yl)methanone (22 mg, 46% yield) as a light yellow solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.46 (s, 1H), 7.93-7.87 (m, 2H), 7.74-7.65 (m, 2H), 2.56 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₂ H ₁₀ BClN ₃ O ₂ S 306.0, found 306.1. HPLC purity: 100% (220 nm), 100% (254 nm). [0361] Example 58: (6-chloro-1-hydroxy-2,3,1-benzo-diazaborinin-2-yl)-[3-(diflu oro methyl)-1-methyl-pyrazol-4-yl]methanone [0362] To a solution of 3-(difluoromethyl)-1-methyl-pyrazole-4-carboxylic acid (500 mg, 2.84 mmol, 1 eq) in DCM (8 mL) was added EDCI (653 mg, 3.41 mmol, 1.2 eq), TEA (861 mg, 8.52 mmol, 1.19 mL, 3 eq) and HOBt (422 mg, 3.12 mmol, 1.1 eq), then tert-butyl N- aminocarbamate (413 mg, 3.12 mmol, 1.1 eq) was added. The mixture was stirred at 25°C for 12 hours. H ₂ O (10 mL) was added and the mixture was extracted with EtOAc (10 mL x 3). The combined organic phase was dried over anhydrous Na2SO4, filtered, and concentrated in vacuo to give a residue, which was purified by flash silica gel chromatography (ISCO®; 20 g SepaFlash® Silica Flash Column, Eluent of 0 → 30% ethyl acetate/Petroleum ether gradient @50 mL/min) to give tert-butyl N-[[3-(difluoromethyl)-1-methyl-pyrazole-4-carbonyl]amino] carbamate (255 mg, 31% yield) as a yellow solid. ¹ H NMR (CDCl _3, 400 MHz) δ 9.94 (s, 1H), 8.86 (s, 1H), 8.23 (s, 1H), 7.26 (t, J = 54.0 Hz, 1H), 3.91 (s, 3H), 1.39 (s, 9H). [0363] To a solution of tert-butyl N-[[3-(difluoromethyl)-1-methyl-pyrazole-4-carbonyl]- amino]carbamate (0.2 g, 689.02 µmol, 1 eq) in EtOAc (2 mL) was added HCl/EtOAc (4 M, 1.72 mL, 10 eq). The mixture was stirred at room temperature for 1 hour, and then concentrated in vacuo to give 3-(difluoromethyl)-1-methyl-pyrazole-4-carbohydrazide (0.2 g, crude) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 8.40-8.33 (m, 1H), 7.26 (t, J = 54.0 Hz, 1H), 3.95 (s, 3H). [0364] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (116 mg, 631.08 µmol, 1.2 eq) and 3-(difluoromethyl)-1-methyl-pyrazole-4-carbohydrazide (100 mg, 525.90 µmol, 1 eq) in EtOH (2 mL) was added NH3-H ₂ O (442 mg, 3.16 mmol, 486.08 µL, 25% purity, 6 eq). The mixture was stirred at 50°C for 2 hours. H ₂ O (10 mL) was added to the mixture, and the formed precipitate was collected by filtration, washed with H ₂ O (5 mL), and dried in vacuo to give (6- chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-[3-(difluoro methyl)-1-methyl-pyrazol-4- yl]methanone (62 mg, 28% yield) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.82 (s, 1H), 8.26 (s, 1H), 7.85 (s, 1H), 7.68 (d, J = 7.6 Hz, 1H), 7.58 (dd, J = 7.6Hz, 2.0 Hz, 1H), 6.60 (t, J = 54.0 Hz, 1H), 3.94 (s, 3H). MS (ESI) (m/z): [M-H]- calculated for C13H9BClF2N4O2337.1, found 337.0. HPLC purity: 79.97% (220 nm), 83.45% (254 nm). [0365] (6-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(2-c hlorophenyl) methanethione [0366] To a suspension of (4-chloro-2-formyl-phenyl)boronic acid (0.9 mmol, 1 equivalent) and 2-chloro-benzothiohydrazide (0.9 mmol, 1 equivalent) in ethanol were added a few drops of ammonium hydroxide and the resulting mixture was stirred at 60 °C for 2 hours. The formed solid was filtered and washed with ethanol, then purified using prep-HPLC to give the desired product as a yellow solid (33 mg, 11% yield). ¹ H NMR (CDCl _3, 400 MHz) δ 7.61 (d, J = 8.0 Hz, 1H), 7.46-7.45 (m, 2H), 7.37-7.35 (m, 1H), 7.27-7.24 (m, ₂ H), 7.18 (s, 1H), 6.57 (s, 1H). MS (ESI) (m/z): [M+H] ⁺ calculated for C ₁₄ H ₁₀ BCl ₂ N ₂ OS 335.0, found 335.0. HPLC purity: 93.3% (220 nm), 98.2% (254 nm). [0367] Example 59: (1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(1-methyl-1H- imidazol-2-yl)methanone [0368] This substance was prepared by using General Procedure as a white solid. Yield: 37%. ¹ HNMR (400 MHz, DMSO-d6): δ 7.91 (dd, J = 8.1, 3.6 Hz, 2H), 7.48-7.31 (m, 2H), 7.31- 7.20 (m, ₂ H), 6.76 (d, J = 1.5 Hz, 1H), 3.79 (s, 3H) ppm. MS (ESI) (m/z): [M+H] ⁺ calculated for C1 ₂ H12BN4O2255.1, found 255.1. [0369] Example 60 (6-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl)(3- (difluoromethyl)-1-methyl-1H-pyrazol-4-yl)methanone [0370] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (116 mg, 631.08 µmol, 1.2 eq) and 3-(difluoromethyl)-1-methyl-pyrazole-4-carbohydrazide (100 mg, 525.90 µmol, 1 eq) in EtOH (2 mL) was added NH3 ^. H ₂ O (442 mg, 3.16 mmol, 486.08 µL, 25% purity, 6 eq). The resulting mixture was stirred at 50°C for 2 h. H ₂ O (10 mL) was added to the mixture, and the precipitate was collected by filtration, washed with H ₂ O (5 mL), dried in vacuum to give (6- chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-[3-(difluoro methyl)-1-methyl-pyrazol-4- yl]methanone (62 mg, 147.42 µmol, 28.03% yield, 79.97% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.82 (s, 1H), 8.26 (s, 1H), 7.85 (s, 1H), 7.68 (d, J = 7.6 Hz, 1H), 7.58 (dd, J = 7.6Hz, 2.0 Hz, 1H), 6.60 (t, J = 54.0 Hz, 1H), 3.94 (s, 3H). MS (ESI): mass calcd. For C13H10BClF2N4O2338.06, m/z found 337.0 [M-H]-. HPLC: 79.97% (220 nm), 83.45% (254 nm). [0371] Example 611-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-2-meth yl- propan- 1-one [0372] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (200 mg, 1.08 mmol, 1 eq) and 2-methylpropanehydrazide (111 mg, 1.08 mmol, 1 eq) in EtOH (5 mL) was added NH ₃ .H ₂ O (1.95 mmol, 301 µL, 25% purity, 1.8 eq) dropwise at room temperature, the resulting mixture was stirred at 50 ^o C for 1 h. The reaction mixture was concentrated in vacuo to give crude product, which was triturated with H ₂ O (6 mL)/acetonitrile (2 mL) (v:v=3:1) at room temperature to afford 1-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-2-methyl -propan- 1-one (100 mg, 388 µmol, 35.76% yield, 97.15% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.19 (s, 1H), 7.74 (d, J = 2.0 Hz, 1H), 7.62-7.60 (m, 1H), 7.57-7.55 (m, 1H), 3.81- 3.78 (m, 1H).1.01 (d, J = 6.8 Hz, 3H), 0.96 (d, J = 6.8 Hz, 3H). MS (ESI): mass calcd. For C11H12BClN ₂ O2250.07, m/z found 267.1 [M+18-H]-. HPLC: 97.15% (220 nm), 97.02% (254 nm). [0373] Example 62 (6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl) -(2- hydroxycyclopentyl)methanone [0374] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (64 mg, 347 µmol, 1 eq) and 2-hydroxycyclopentanecarbohydrazide (50 mg, 347 µmol, 1 eq) in EtOH (1.5 mL) was added NH ₃ .H ₂ O (649 µmol, 100 µL, 25% purity, 1.87 eq) dropwise at 25°C, the resulting mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated in vacuo to give a residue, which was purified by prep-HPLC (column: Waters Xbridge 150*255u;mobile phase: [water(10mM NH ₄ HCO ₃ )-ACN]; B%: 1%-30%,20min) to give (6-chloro-1-hydroxy-2,3,1- benzodiazaborinin-2-yl)-(2-hydroxycyclopentyl)methanone (20 mg, 64.2 µmol, 18.51% yield, 93.88% purity) as a white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 7.70 (br s, 1H), 7.52 (d, J = 7.6 Hz, 1H), 7.39 (br s, 1H), 7.36-7.34 (m, 1H), 6.13-5.98 (m, 1H), 3.70-3.67 (m, 1H), 1.92- 1.89 (m, 1H), 1.79-1.69 (m, ₂ H), 1.60-1.49 (m, 4H). MS (ESI): mass calcd. For C13H14ClN ₂ O3 292.08, m/z found 291.0 [M-H]-. HPLC: 93.88% (220 nm), 93.93% (254 nm). [0375] Example 63 (6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl) -cyclohexyl- methanone [0376] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (200 mg, 1.08 mmol, 1 eq) and cyclohexanecarbohydrazide (154 mg, 1.08 mmol, 1 eq) in EtOH (4 mL) was added NH ₃ .H ₂ O (1.95 mmol, 0.3 mL, 25% purity, 1.80 eq) dropwise at 25°C, the resulting mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated in vacuo to give a residue,, which was purified by prep-HPLC (column: Waters Xbridge 150*255u; mobile phase: [water(0.04%NH3H ₂ O)-ACN]; B%: 20%-50%,20min) to give (6-chloro-1-hydroxy-2,3,1- benzodiazaborinin-2-yl)-cyclohexyl –methanone (70 mg, 236µmol, 21.89% yield, 98.14% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.18 (s, 1H), 7.74 (s, 1H), 7.60-7.58 (m, 1H), 7.56-7.54 (m 1H), 3.57-3.51 (m, 1H), 1.71-1.56 (m, 5H), 1.25-1.06 (m, 5H). MS (ESI): mass calcd. For C14H16ClN ₂ O3290.10, m/z found 289.1 [M-H]-. HPLC: 98.14% (220 nm), 97.75% (254 nm). [0377] Example 64 1-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-2-methyl - butan-1 -one [0378] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (80 mg, 430 µmol, 1 eq) and 2-methylbutanehydrazide (50 mg, 430 µmol, 1 eq) in EtOH (2 mL) was added NH ₃ .H ₂ O (649µmol, 0.1 mL, 25% purity, 1.50 eq) dropwise at 25°C, the resulting mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated in vacuo to give a residue, which was purified by prep-HPLC (column: Waters Xbridge 150*255u; mobile phase: [water(0.04%NH3H ₂ O)-ACN]; B%: 5%-25%,20min) to give 1-(6-chloro-1-hydroxy-2,3,1- benzodiazaborinin-2-yl)-2-methyl- butan-1-one (34 mg, 112.78 µmol, 26.20% yield, 87.74% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.20-8.17 (m, 1H), 1.95 (m, 3H), 0.78- 0.70 (m, 3H), MS (ESI): mass calcd. For C1 ₂ H14BClN ₂ O2264.08, m/z found 263.1 [M-H]-. HPLC: 87.75% (220 nm), 85.14% (254 nm). [0379] Example 651-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)butan-1 -one [0380] To a solution of (4-chloro-2-formyl-phenyl)boronic acid (200 mg, 1.08 mmol, 1 eq) in EtOH (2 mL) was added NH ₃ .H ₂ O (274 mg, 1.95 mmol, 2.17 µL, 25% purity, 1.8 eq) and butanehydrazide (111 mg, 1.08 mmol, 1 eq), the resulting mixture was stirred at 50°C for 2 h. The reaction was quenched by adding ice-water (20 mL) at 0°C, and the precipitate was collected by filtration, which was triturated with H ₂ O (6 mL)/acetonitrile (2 mL)(v:v=3:1 ) at 25 ^o C for 10 min to give 1-(6-chloro-1-hydroxy-2,3,1-benzodiazab orinin-2-yl)butan-1-one (185 mg, 738.56 µmol, 68.09% yield) as a white solid. ¹ HNMR (DMSO-d6, 400 MHz) δ 8.17 (s, 1H), 7.74 (d, J = 2.0 Hz, 1H), 7.61 (d, J = 8.0 Hz, 1H), 7.56 (dd, J = 8.0 Hz, J = 2.0 Hz, 1H), 2.86-2.77 (m, 2H), 1.53-1.46 (m, ₂ H), 0.81 (t, J = 7.2 Hz, 3H). MS (ESI): mass calcd. For C11H12BClN ₂ O2 250.07 m/z found 249.1 [M-H]-. HPLC: 99.14% (220 nm), 99.40% (254 nm). [0381] Example 66.1-(6-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl )-3- hydroxy-4-methylpentan-1-one [0382] Example 67 Preparation of methyl 3-hydroxy-4-methyl-pentanoate [0383] To a solution of methyl 4-methyl-3-oxo-pentanoate (2.07 g, 12.64 mmol, 2.0 mL, 1 eq) in HF (20 mL)/MeOH (1 mL) was added NaBH4 (957 mg, 25.29 mmol, 2 eq) dropwise at 0 ^o C, the resulting mixture was stirred at 0°C for 1 h. The reaction was quenched by 1 N HCl (30 mL) at 0°C, and the aqueous phase was extracted with EtOAc (20 mL x 3). The combined organic layers were washed with brine (30 mL x 2), dried over Na2SO4, filtered and concentrated in vacuo to give methyl 3-hydroxy-4-methyl-pentanoate (2.00 g, crude), which was used directly in next step without further purification. [0384] Example 68 Preparation of 3-hydroxy-4-methyl-pentanehydrazide [0385] To a solution of methyl 3-hydroxy-4-methyl-pentanoate (2.00 g, 13.68 mmol, 1 eq) in EtOH (20 mL) was added NH ₂ NH ₂ .H ₂ O (2.05 g, 41.04 mmol, 2.0 mL, 3 eq), the resulting mixture was stirred at 90°C for 12 h. Then the reaction mixture was partitioned between H ₂ O (30 mL) and EtOAc (30 mL), and the organic phase was separated, washed with brine (30 mL x 2), dried over Na2SO4, filtered and concentrated in vacuo to give 3-hydroxy-4-methyl- pentanehydrazide (2.00 g, crude) as a white solid, which was used directly in the next step without further purification. ¹ HNMR (DMSO-d _6, 400 MHz) δ 4.02-3.82 (m, 1H), 3.69-3.61 (m, 1H), 3.35 (s, 3H), 2.28-2.14 (m, 1H), 1.75-1.58 (m, 2H), 0.95-0.83 (m, 6H). [0386] Example 69 Preparation of 1-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinin- 2-yl)-3-hydroxy-4- methyl-pentan-1-one [0387] To a solution of 3-hydroxy-4-methyl-pentanehydrazide (175 mg, 1.2 mmol, 1.1 eq) and (4-chloro-2-formyl-phenyl)boronic acid (200 mg, 1.08 mmol, 1 eq) in EtOH (2 mL) was added NH ₃ .H ₂ O (114 mg, 3.25 mmol, 126 µL, 3 eq), the resulting mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated in vacuo to give a residue, which was purified by prep-HPLC (column: Welch Xtimate C ₁₈ 150*25mm*5um; mobile phase: [water(10mM NH4HCO ₃ )-ACN]; B%: 15%-45%,10.5min) to give 1-(6-chloro-1-hydroxy-2,3,1- benzodiazaborinin-2-yl)-3-hydroxy-4-methyl-pentan-1-one (120 mg, 407.41 µmol, 37.56% yield) as a white solid. ¹ HNMR (DMSO-d6, 400 MHz) δ 8.11 (s, 1H), 7.87 (d, J = 8.0 Hz, 1H), 7.80 (d, J = 2.0 Hz, 1H), 7.62 (dd, J = 8.0 Hz, J = 2.0 Hz, 1H), 5.44 (br s, 1H), 4.10-4.00 (m, 1H), 2.76-2.64 (m, 1H), 2.63-2.56 (m, 1H), 1.81-1.75 (m, 1H), 0.98 (d, J = 7.2 Hz, 3H), 0.93 (d, J = 7.2 Hz, 3H). MS (ESI): mass calcd. For C13H16BClN ₂ O3294.09 m/z found 277.0 [M-OH] ⁺ . HPLC: 99.31% (220 nm), 99.26% (254 nm). [0388] Example 701-(6-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin-2(1H)-yl) -2- phenylethan-1-one [0389] A mixture of (4-chloro-2-formyl-phenyl)boronic acid (250 mg, 1.36 mmol, 1 eq), 2- phenylacetohydrazide (204 mg, 1.36 mmol, 1 eq) and NH ₃ .H ₂ O (380 mg, 2.71 mmol, 25% purity, 2 eq) in EtOH (5 mL) was degassed and purged with N ₂ for 3 times, the resulting mixture was stirred at 60°C for 2 h under N ₂ atmosphere. The reaction mixture was concentrated in vacuo to give the crude product. The crude product was triturated with EtOH (2 mL) at 25 ^o C for 15 min to give 1-(6-chloro-1-hydroxy -2,3,1-benzodiazaborinin-2-yl)-2-phenyl-ethanone (134 mg, 32.5% yield, 98.04% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.19 (s, 1H), 7.73 (s, 1H), 7.58-7.49 (m, ₂ H), 7.28-7.20 (m, 3H), 7.11 (d, J = 6.4 Hz, 2H), 4.33 (d, J = 13.6 Hz, 1H), 4.06 (d, J = 13.6 Hz, 1H). MS (ESI): mass calcd. For C ₁₅ H ₁₂ BClN ₂ O ₂ 298.07, m/z found 299.1 [M+H] ⁺ . HPLC: 98.04% (220 nm), 96.32% (254 nm). [0390] Example 71.3-(6-chloro-1-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazabori nine- 2-carbonyl)-1-cyclopropylquinolin-4(1H)-one

[0391] Example 72 Preparation of ethyl 3-(dimethylamino)-2-(2- fluorobenzoyl)acrylate [0392] A mixture of ethyl 3-(2-fluorophenyl)-3-oxo-propanoate (4.00 g, 19.0 mmol, 3.5 mL, 1 eq) and DMF-DMA (3.40 g, 28.5 mmol, 3.8 mL, 1.5 eq) in toluene (50 mL) was refluxed at 120 ^o C for 2 h. The reaction mixture was cooled to room temperature, concentrated in vacuo to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~50% Ethylacetate/Petroleum ethergradient @ 75 mL/min) to give ethyl 3-(dimethylamino)-2-(2-fluorobenzoyl)acrylate (4.80 g, 95.1% yield) as yellow oil, which was used directly in the next step without further purification. [0393] Example 73 Preparation of ethyl 1-cyclopropyl-4-oxo-quinoline-3- carboxylate [0394] A mixture of ethyl 3-(dimethylamino)-2-(2-fluorobenzoyl)acrylate (2.50 g, 9.42 mmol, 1 eq) and cyclopropanamine (592 mg, 10.4 mmol, 718 µL, 1.1 eq) in DMF (20 mL) was refluxed (140°C) for 16 h. The reaction was quenched by adding water (60 mL) at 0°C, the resulting mixture was diluted with EtOAc (20 mL), and the aqueous phase was extracted with EtOAc (30 mL x 3). The combined organic layers were washed with brine (40 mL x 3), dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give crude product. The crude product was triturated with MTBE (25 mL) at 25 ^o C for 20 min to give ethyl 1-cyclopropyl-4- oxo-quinoline-3-carboxylate (0.75 g, 30.9% yield) as a white solid. ¹ H NMR (CDCl _3, 400 MHz) δ 8.63 (s, 1H), 8.52 (dd, J = 1.6, 8.0 Hz, 1H), 7.94 (d, J = 8.4 Hz, 1H), 7.72 (t, J = 7.6 Hz, 1H), 7.47 (t, J = 7.6 Hz, 1H), 4.41 (q, J = 7.2 Hz, 2H), 3.58-3.40 (m, 1H), 1.42 (t, J = 7.2 Hz, 3H), 1.37-1.33 (m, 2H), 1.22-1.09 (m, ₂ H). [0395] Example 74 Preparation of 1-cyclopropyl-4-oxo-quinoline-3-carbohydrazide [0396] A mixture of ethyl 1-cyclopropyl-4-oxo-quinoline-3-carboxylate (200 mg, 777 µmol, 1 eq), N ₂ H4.H ₂ O (397 mg, 7.77 mmol, 10 eq) in EtOH (3 mL) was stirred at 88°C for 12 h under N ₂ atmosphere. The reaction mixture was cooled to room temperature, and the precipitate was collected by filtration, washed with MTBE (3 mL) to give 1-cyclopropyl-4-oxo- quinoline -3-carbohydrazide (180 mg, 95.2% yield) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 10.59 (br s, 1H), 8.70 (s, 1H), 8.33 (dd, J = 1.6, 8.0 Hz, 1H), 8.17 (d, J = 8.4 Hz, 1H), 7.92-7.87 (m, 1H), 7.56 (t, J = 7.6 Hz, 1H), 4.59 (br d, J = 4.4 Hz, ₂ H), 3.80-3.73 (m, 1H), 1.35- 1.26 (m, 2H), 1.17-1.05 (m, ₂ H). [0397] Example 75 Preparation of 3-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinine- 2-carbonyl)-1- cyclopropyl-quinolin-4-one [0398] A mixture of (4-chloro-2-formyl-phenyl)boronic acid (76 mg, 411 µmol, 1 eq), 1- cyclopropyl-4-oxo-quinoline-3-carbohydrazide (100 mg, 411 µmol, 1 eq) and NH ₃ .H ₂ O (346 mg, 2.47 mmol, 380 µL, 25% purity, 6 eq) in EtOH (3 mL) was degassed and purged with N ₂ for 3 times, the resulting mixture was stirred at 70°C for 12 h under N ₂ atmosphere. The reaction mixture was cooled to room temperature, concentrated in vacuo to give the crude product. The crude product was triturated with CH ₃ CN (2 mL) and water (3 mL) at 25 ^o C for 15 min to give 3- (6-chloro-1-hydroxy-2,3,1-benzodiazaborinine-2-carbonyl)-1-c yclopropyl-quinolin-4-one (116 mg, 71.2% yield, 98.76% purity) as a white solid. ¹ H NMR (DMSO-d _6, 400 MHz) δ 9.24 (s, 1H), 8.71 (d, J = 8.4 Hz, 1H), 8.57 (d, J = 8.8 Hz, 1H), 8.22 (t, J = 7.2 Hz, 1H), 7.99-7.91 (m, 2H), 7.86 (s, 1H), 7.54-7.46 (m, 2H), 4.24-4.13 (m, 1H), 3.57 (s, 1H), 1.51-1.39 (m, 3H), 1.25- 1.23 (m, 1H). MS (ESI): mass calcd. For C ₂₀ H ₁₅ BClN ₃ O ₃ 391.09, m/z found 392.1 [M+H] ⁺ . HPLC: 98.76% (220 nm), 99.01% (254 nm). [0399] Example 76.3-(6-chloro-1-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazabori nine- 2-carbonyl)-1-ethylquinolin-4(1H)-one [0400] Example 77 Preparation of ethyl 1-ethyl-4-oxo-quinoline-3-carboxylate [0401] To a mixture of ethyl 4-oxo-1H-quinoline-3-carboxylate (2.00 g, 9.21 mmol, 1 eq) in DMF (20 mL) was added K ₂ CO ₃ (2.54 g, 18.41 mmol, 2 eq) and iodoethane (4.31 g, 27.62 mmol, 2.21 mL, 3 eq) at 25°C, the resulting mixture was stirred at 80°C for 4 h. Then the reaction mixture was cooled to 25°C, poured into iced sat. NH4Cl (20 mL), and the aqueous phase was extracted with EtOAc (15 mL x 3). The combined organic phase was washed with brine (15 mL x 2), dried over anhydrous Na2SO4, filtered and concentrated in vacuo to give a residue. The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=1/4 to 0/1) to give ethyl 1-ethyl-4-oxo-quinoline-3-carboxylate (1.80 g, 7.34 mmol, 79.71% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 8.57 (dd, J = 8.0, 1.2 Hz, 1H), 8.52 (s, 1H), 7.72-7.68 (m, 1H), 7.48-7.43 (m, ₂ H), 4.41 (q, J = 7.2 Hz, 2H), 4.27 (q, J = 7.2 Hz, ₂ H), 1.56 (t, J = 7.2 Hz, 3H), 1.43 (t, J = 7.2 Hz, 3H). [0402] Example 78 Preparation of 1-ethyl-4-oxo-quinoline-3-carbohydrazide [0403] To a solution of ethyl 1-ethyl-4-oxo-quinoline-3-carboxylate (1.50 g, 6.12 mmol, 1 eq) in EtOH (20 mL) was added NH ₂ NH ₂ .H ₂ O (469 mg, 9.17 mmol, 455 µL, 98% purity, 1.5 eq) at 25°C, the resulting mixture was stirred at 90°C for 6 h. The reaction mixture was cooled to room temperature, concentrated in vacuo to a residue, which was dissolved in MTBE, the resulting mixture was stirred at room temperature for 15 min. The precipitate from the mixture was collected by filtration, washed with MTBE (10 mL), and dried in vacuo to give 1-ethyl-4- oxo-quinoline-3-carbohydrazide (860 mg, 3.72 mmol, 60.81% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.88 (s, 1H), 8.36 (d, J = 7.2 Hz, 1H), 7.93-7.90 (m, 1H), 7.87-7.84 (m, 1H), 7.54 (t, J = 7.2 Hz, 1H), 4.59 (br s, 2H), 4.52 (q, J = 7.2 Hz, ₂ H), 1.39 (t, J = 7.2 Hz, 3H). [0404] Example 79 Preparation of 3-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinine- 2-carbonyl)-1-ethyl-quinolin-4-one [0405] To a mixture of 1-ethyl-4-oxo-quinoline-3-carbohydrazide (139 mg, 601 µmol, 1 eq) and (4-chloro-2-formyl-phenyl)boronic acid (111 mg, 601 µmol, 1 eq) in EtOH (5 mL) was added NH ₃ .H ₂ O (182 mg, 1.04 mmol, 0.2 mL, 20% purity, 1.73 eq) in one portion at 25°C, the resulting mixture was stirred at 25°C for 0.5 h. The reaction mixture was concentrated in vacuo to give a residue. The residue was purified by prep-HPLC (column: Welch Xtimate C18 150*25mm*5um;mobile phase: [water(10mM NH ₄ HCO ₃ )-ACN]; B%:30%-60%,10.5min) to give 3-(6-chloro-1-hydroxy-2,3,1-benzodiazaborinine-2-carbonyl)-1 -ethyl-quinolin-4-one (48 mg, 124 µmol, 20.67% yield, 98.24% purity) obtained as a white solid . ¹ H NMR (DMSO-d6, 400 MHz) δ 9.60 (s, 1H), 8.74 (dd, J = 8.4, 1.6 Hz, 1H), 8.37 (d, J = 9.2 Hz, 1H), 8.21 (t, J = 8 Hz, 1H), 7.98-7.95 (m, , 2H), 7.86 (s, 1H), 7.51-7.47 (m, ₂ H), 4.93 (q, J = 7.2 Hz, 2H), 1.53 (t, J = 7.2 Hz, 3H). MS (ESI): mass calcd. For C19H15BClN3O3, 379.6, m/z found 380.2 [M+H] ⁺ . HPLC: 98.24% (220 nm), 99.29 (254 nm). [0406] Example 80. Preparation of 1-ethyl-3-(6-fluoro-1-hydroxy-2,3,1- benzodiazaborinine-2-carbonyl)quinolin-4-one 123 [0407] To a mixture of 1-ethyl-4-oxo-quinoline-3-carbohydrazide (200 mg, 865 µmol, 1 eq) in EtOH (5 mL) was added (4-fluoro-2-formyl-phenyl)boronic acid (145 mg, 865 µmol, 1 eq) and NH ₃ .H ₂ O (270 mg, 1.54 mmol, 297 µL, 20% purity, 1.78 eq) in one portion at 25°C, the resulting mixture was stirred at 25°C for 0.5 h. The reaction mixture was concentrated in vacuo to give a residue. The residue was purified by prep-HPLC (column: Welch Xtimate C18 150*25mm*5um;mobile phase: [water(10mM NH ₄ HCO ₃ )-ACN]; B%: 20%-50%,10.5min) to give 1-ethyl-3-(6-fluoro-1-hydroxy-2,3,1-benzodiazaborinine-2-car bonyl)quinolin-4-one (225 mg, 598 µmol, 69.12% yield, 96.49% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 9.60 (s, 1H), 8.74 (d, J = 6.8 Hz, 1H), 8.36 (d, J = 8.8 Hz, 1H), 8.18 (t, J = 7.2 Hz, 1H), 8.09-7.90 (m, 2H), 7.85 (s, 1H), 7.28-7.24 (m, ₂ H), 4.93 (q, J = 6.8 Hz, 2H), 1.53 (t, J = 6.8 Hz, 3H). MS (ESI): mass calcd. For C19H15BFN3O3, 363.15, m/z found 364.2 [M+H] ⁺ . HPLC: 96.49% (220 nm), 97.99 (254 nm). [0408] Example 81 Preparation of 1-ethyl-3-(1-hydroxy-2,3,1-benzodiazaborinine-2- carbonyl)quinolin-4-one [0409] To a mixture of 1-ethyl-4-oxo-quinoline-3-carbohydrazide (200 mg, 865 µmol, 1 eq) in EtOH (5 mL) was added NH ₃ .H ₂ O (273 mg, 7.78 mmol, 300 µL, 9 eq) and (2- formylphenyl)boronic acid (130 mg, 865 µmol, 1 eq) in one portion at 25°C, the resulting mixture was stirred at 25°C for 0.5 h. The reaction mixture was concentrated in vacuo to give a residue. The residue was purified by prep-HPLC (column: Welch Xtimate C18150*25mm*5um; mobile phase: [water(10mM NH4HCO3)-ACN]; B%: 20%-50%,10.5min) to give 1-ethyl-3-(1-hydroxy- 2,3,1-benzodiazaborinine-2-carbonyl)quinolin-4-one (180 mg, 512 µmol, 59.23% yield, 98.22% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 9.59 (s, 1H), 8.74 (d, J = 8.4 Hz, 1H), 8.35 (d, J = 8.8 Hz, 1H), 8.18 (t, J = 8 Hz, 1H), 7.97 (d, J = 6.8 Hz, 1H), 7.94 (t, J = 8.0 Hz, 1H), 7.85 (s, 1H), 7.45 (t, J = 7.2 Hz, 1H), 7.41-7.35 (m, 2H), 4.92 (q, J = 7.2 Hz, ₂ H), 1.53 (t, J = 7.2 Hz, 3H). MS (ESI): mass calcd. For C19H16BN3O3, 345.16, m/z found 344.0 [M-H]-. HPLC: 98.22% (220 nm), 98.67 (254 nm). [0410] Example 82. Preparation of (6-chloro-1-hydroxybenzo[d][1,2,3]diazaborinin- 2(1H)-yl)(pyridin-2-yl)methanone [0411] A mixture of (4-chloro-2-formyl-phenyl)boronic acid (200 mg, 1.08 mmol, 1 eq) and pyridine-2-carbohydrazide (163 mg, 1.19 mmol, 1.1 eq) in EtOH (10 mL) was degassed and purged with N ₂ for 3 times, then the reaction mixture was stirred at 20°C for 2 h under N ₂ atmosphere. The yellow solid from the mixture was collected by filtration, washed with EtOH (1 mL x 2), and dried in vacuo to give (6-chloro-1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-(2- pyridyl)methanone (50 mg, 175.14 µmol, 16.22% yield) as a yellow solid. ¹ H NMR (DMSO- d6+D2O, 400 MHz) δ 9.28 (d, J = 5.2 Hz, 1H), 8.54 (t, J = 7.2 Hz, 1H), 8.21 (d, J = 7.6 Hz, 1H), 8.13 (t, J = 7.2 Hz, 1H), 8.06 (s, 1H), 7.80 (d, J = 8.0 Hz, 1H), 7.59 (d, J = 2.4 Hz, 1H), 7.46 (dd, J = 8.0 Hz, 2.4 Hz, 1H). MS (ESI): mass calcd. For C13H9BClN3O2285.05, m/z found 284.0 [M- H]-. HPLC: 100% (220 nm), 99.81% (254 nm). [0412] Example 83. Preparation of (E)-1-(1-hydroxy-2,3,1-benzodiazaborinin-2-yl)- 3-phenyl-prop-2-en-1-one [0413] Example 84 Preparation of tert-butyl N-[[(E)-3-phenylprop-2- enoyl]amino]carbamate [0414] To a solution of (E)-3-phenylprop-2-enoic acid (5.00 g, 33.75 mmol, 4.00 mL, 1 eq)，EDCI (7.76 g, 40.50 mmol, 1.2 eq)，HOBT (5.02 g, 37.12 mmol, 1.1 eq) and TEA (10.24 g, 101.24 mmol, 14.10 mL, 3 eq) in DCM (50 mL) was added tert-butyl N-aminocarbamate (4.91 g, 37.12 mmol, 1.1 eq) in portions at 20°C, the resulting mixture was stirred at 20°C for 16 h. The reaction mixture was diluted with H ₂ O (30 mL), and the aqueous phase was extracted with EtOAc (25 mL x 3). The combined organic phase was washed with brine (25 mL x 2), dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give a residue, which was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=3/1 to 1/3) to afford tert-butyl N-[[(E)-3-phenylprop-2-enoyl] amino]carbamate (7.10 g, 27.07 mmol, 80.21% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 8.47 (br s, 1H), 7.67 (d, J = 15.6 Hz, 1H), 7.44-7.42 (m, ₂ H), 7.34-7.31 (m, 3H), 7.08 (br s, 1H), 6.49 (d, J = 15.6 Hz, 1H), 1.46 (s, 9H). [0415] Example 85 Preparation of (E)-3-phenylprop-2-enehydrazide [0416] To a mixture of tert-butyl N-[[(E)-3-phenylprop-2-enoyl]amino]carbamate (500 mg, 1.91 mmol, 1 eq) in DCM (10 mL) was added TFA (2 mL) dropwise at 25°C, the resulting mixture was stirred at 25 °C for 1 h. The reaction mixture was concentrated in vacuo to give (E)-3-phenylprop-2-enehydrazide (300 mg, crude, TFA salt) as a colorless liquid, which was used directly in the next step. [0417] Example 86 Preparation of (E)-1-(1-hydroxy-2,3,1-benzodiazaborinin-2-yl)-3- phenyl-prop-2-en-1-one [0418] To a mixture of (E)-3-phenylprop-2-enehydrazide TFA salt (300 mg, 1.09 mmol, 1 eq) in EtOH (7 mL) was added NH ₃ .H ₂ O (423 mg, 3.26 mmol, 465 µL, 27% purity, 3 eq) and (2- formylphenyl)boronic acid (163 mg, 1.09 mmol, 1 eq) at 25°C, the resulting mixture was stirred at 25°C for 0.5 h. The reaction mixture was concentrated in vacuo to give a residue. The residue was triturated with DMF/H ₂ O (3 mL/0.5 mL) to give (E)-1-(1-hydroxy-2,3,1- benzodiazaborinin-2-yl)-3-phenyl-prop-2-en-1-one (48 mg, 174 µmol, 16.01% yield, 96.88% purity) as a white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 7.90 (d, J = 16.0 Hz, 1H), 7.88-7.64 (m, 3H), 7.54 (s, 1H), 7.50-7.48 (m, 1H), 7.43-7.38 (m, 3H), 7.27-7.22 (m, 3H). MS (ESI): mass calcd. For C16H13BN ₂ O2, 276.11, m/z found 277.1 [M+H] ⁺ . HPLC: 96.88% (220 nm), 97.72 (254 nm). [0419] Exanple 87 Preparation of (8,9-dihydro-1H-7,10-dioxa-1,2-diaza-10a- boracyclohepta[de] naphthalen-1-yl)(phenyl)methanone [0420] Example 88 Preparation of 2-bromo-3-[2-[tert-butyl(dimethyl)silyl]- oxyethoxy]benzaldehyde [0421] To a mixture of 2-bromo-3-hydroxy-benzaldehyde (5.00 g, 24.9 mmol, 1 eq) and 2-bromoethoxy-tert-butyl-dimethyl-silane (7.14 g, 29.9 mmol, 1.2 eq) in DMF (100 mL) was added K ₂ CO ₃ (8.59 g, 62.2 mmol, 2.5 eq) in one portion at 25°C under N ₂ atmosphere, the resulting mixture was heated to 90°C and stirred for 3 h. Sat. aq. NH ₄ Cl (200 mL) was then added into the above mixture, the aqueous phase was extracted with EtOAc (50 mL x 3). The combined organic layers were washed with brine (100 mL x 2), dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give a residue. The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 2-bromo-3-[2-[tert- butyl(dimethyl)silyl]oxyethoxy]benzaldehyde (8.00 g, 22.3 mmol, 89.5% yield) as yellow oil. 1H NMR (CDCl ₃ , 400 MHz) δ 10.32 (s, 1H), 7.41 (d, J = 7.2 Hz, 1H), 7.23 (t, J = 8.0 Hz, ₂ H), 7.06 (d, J = 8.0 Hz, 1H), 4.04 (t, J = 5.2 Hz, 2H), 3.93 (t, J = 5.2 Hz, 2H), 0.79 (s, 9H), 0.00 (s, 6H). [0422] Example 89 Preparation of 3-[2-[tert-butyl(dimethyl)silyl]oxyethoxy]-2-(5,5- dimethyl-1,3,2- dioxaborinan-2-yl)benzaldehyde [0423] To a mixture of 2-bromo-3-[2-[tert-butyl(dimethyl)silyl]oxyethoxy]benzaldehy de (3.50 g, 9.74 mmol, 1 eq) and 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-5,5-dimethyl-1,3,2- dioxaborinane (5.50 g, 24.4 mmol, 2.5 eq) in 1,4-dioxane (50 mL) was added Pd(PPh ₃ ) ₂ Cl ₂ (0.68 g, 0.97 mmol, 0.1 eq) and KOAc (2.39 g, 24.4 mmol, 2.5 eq) in one portion at 25°C under N ₂ atmosphere, the resulting mixture was heated to 80°C and stirred for 16 h. The reaction mixture was poured into ice-water (w/w = 1/1) (300 mL), the aqueous phase was extracted with ethyl acetate (100 mL x 3). The combined organic phase was washed with brine (100 mL x 2), dried with anhydrous Na2SO4, filtered and concentrated in vacuum to give 3-[2-[tert- butyl(dimethyl)silyl]oxyethoxy]-2-(5,5-dimethyl-1,3,2-dioxab orinan-2-yl)benzaldehyde (3.20 g, 8.16 mmol, 83.7% yield) as yellow oil. ¹ H NMR (CDCI ₃ , 400 MHz) δ 9.93 (s, 1H), 7.44- 7.36 (m, 2H), 7.12 (d, J = 8.4 Hz, 1H), 4.07 (t, J = 6.4 Hz, 2H), 3.94 (t, J = 6.4 Hz, 2H), 3.80 (s, 4H), 1.13 (s, 6H), 0.89 (s, 9H), 0.05 (s, 6H). [0424] Example 90 Preparation of [2-formyl-6-(2-hydroxyethoxy)phenyl]boronic acid [0425] To a mixture of 3-[2-[tert-butyl(dimethyl)silyl]oxyethoxy]-2-(5,5-dimethyl-1 ,3,2- dioxaborinan- 2-yl)benzaldehyde (2.0 g, 5.1 mmol, 1 eq) in CH ₃ CN (30 mL) was added HCl (4 N, 10 mL, 7.85 eq) dropwise at 0°C under N ₂ atmosphere, the resulting mixture was heated to 50°C and stirred for 16 h. The reaction mixture was concentrated in vacuo to give a residue. The residue was purified by prep-HPLC (column: Phenomenex luna C18250*80mm*10 um; mobile phase: [water(0.1%TFA)-ACN]; B%: 1%-20%,20min) to give [2-formyl-6-(2- hydroxyethoxy) phenyl]boronic acid (400 mg, 1.9 mmol, 37.4% yield) as a white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 9.92 (s, 1H), 7.48-7.44 (m, ₂ H), 7.03 (d, J = 7.6 Hz, ₂ H), 6.90 (d, J = 7.6 Hz, ₂ H), 4.03 (t, J = 5.6 Hz, ₂ H), 3.68 (t, J = 5.6 Hz, ₂ H). [0426] Example 91 Preparation of (8,9-dihydro-1H-7,10-dioxa-1,2-diaza-10a- boracyclohepta[de] naphthalen-1-yl)(phenyl)methanone [0427] To a mixture of [2-formyl-6-(2-hydroxyethoxy)phenyl]boronic acid (100 mg, 476 µmol, 1 eq) in EtOH (4 mL) was added benzohydrazide (65 mg, 476 µmol, 1 eq) at 25°C, the resulting mixture was stirred at 25°C for 2 h. The reaction mixture was concentrated in vacuo to give a residue, which was triturated with ethyl acetate (5 mL) at 25 ^o C for 4 min to give (8,9- dihydro-1H-7,10-dioxa-1,2-diaza-10a-boracyclohepta [de]naphthalen-1- yl)(phenyl)methanone (31 mg, 106 µmol, 22.3% yield) as a white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 8.56-8.42 (m, 1H), 7.90 (d, J = 7.2 Hz, 1H), 7.55-7.45 (m, 4H), 7.40-7.38 (m, ₂ H), 7.02-6.97 (m, 1H), 4.55-4.52 (m, 0.5H), 3.93-3.86 (m, 1H), 3.50-3.40 (m, 0.5H), 3.40-3.37 (m, 2H). MS (ESI): mass calcd. For C ₁₆ H ₁₃ BN ₂ O ₃ 292.10, m/z found 293.2 [M+H] ⁺ . [0428] General Procedures. In the schemes, general substitutent groups are represented with assignments that may not align with the formulae of the present disclosure. The following schemes provide variables that should be followed for these schemes and not necessarily applied to the formulae of the present disclosure. [0429] General Procedure F-A for synthesis of 2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)benzaldehyde (4, below) [0430] To a mixture of 5-bromo-2-hydroxy-benzaldehyde (1)(1 eq) and boronic acid (1.5 eq) in H ₂ O was added K ₂ CO ₃ (2 eq) and Tetrakis(triphenylphosphine)palladium (0.0025 eq) at 25°C under N ₂ . The resulting suspension was stirred at 80°C for 6 h. The reaction mixture was cooled, and a precipitate was formed, the precipitate was collected by filtration, washed with water (50 mL) to give the substituted 2-hydroxy-5-phenyl-benzaldehyde (2). [0431] To a mixture of (2) (1 eq) and pyridine (3 eq) in DCM was added Tf ₂ O (1.5 eq) dropwise at 0°C, the resulting mixture was stirred at 0°C for 2 h. The reaction mixture was then poured into sat. aq. NH ₄ Cl, extracted with DCM. The combined organic layers were washed with brine, dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give a residue. The residue was purified by flash silica gel chromatography to give compound (3). [0432] To a solution of compound (3) (1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-1,3,2-dioxaborolane (2 eq) in dioxane was added Pd(dppf)Cl ₂ .CH2Cl ₂ (0.05 eq), KOAc (2 eq) at 25°C, the resulting mixture was stirred at 80°C for 5 h. The reaction mixture was filtered, and the filtrate was concentrated in vacuo to give a residue. The residue was purified by flash silica gel chromatography to give compound (4). [0433] General Procedure F-B for synthesis of acyldiazaborines [0434] To a solution of compound (4) (1 eq) and acylhydrazine (4a) (1 eq) in EtOH was added NH ₃ .H ₂ O (4.00 eq) drop-wise at room temperature. The resulting mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated in vacuo to give a residue, which was triturated in the following solvent systems sequentially: 1. acetonitrile/H ₂ O (v/v = 3/1) at room temperature for 30 min; 2. EtOH at room temperature for 30 min; 3. acetonitrile at room temperature for 30 min; and 4. n-pentane at room temperature for 30 min, to give the acyldiazaborine. [0435] F-1. Preparation of 1-(1-hydroxy-6-phenyl-2,3,1-benzodiazaborinin-2- yl)ethenone [0436] To a mixture of 5-bromo-2-hydroxy-benzaldehyde (10 g, 49.8 mmol, 1 eq) and phenylboronic acid (9.10 g, 74.6 mmol, 1.5 eq) in H ₂ O (350 mL) was added K ₂ CO ₃ (13.8 g, 99.5 mmol, 2 eq) and palladium-triphenylphosphane (0.144 g, 124 umol, 0.0025 eq) at 25°C under N ₂ atmosphere. The resulting suspension was stirred at 80°C for 6 h. The reaction mixture was then cooled to room temperature, the formed precipitate was collected by filtration, washed with water (50 mL), dried in vacuo to give 2-hydroxy-5-phenyl-benzaldehyde (8.3 g, 40.6 mmol, 81.65% yield, 97% purity) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.01 (s, 1H), 10.00 (s, 1H), 7.80-7.78 (m, ₂ H), 7.58-7.56 (m, 2H), 7.47 (t, J = 7.6 Hz, ₂ H), 7.37 (t, J = 7.2 Hz,, 1H), 7.10 (d, J = 8.4 Hz, 1H). [0437] F-1.2 Preparation of (2-formyl-4-phenyl-phenyl) trifluoromethanesulfonate [0438] To a mixture of 2-hydroxy-5-phenyl-benzaldehyde (7 g, 35.3 mmol, 1 eq) and pyridine (106 mmol, 8.55 mL, 3 eq) in DCM (100 mL) was added Tf ₂ O (53.0 mmol, 8.74 mL, 1.5 eq) dropwise at 0°C, the resulting mixture was stirred at 0°C for 2 h. The reaction mixture was then poured into sat. aq. NH ₄ Cl (150 mL), the aqueous phase was extracted with DCM (80 mL x 3). The combined organic layers were washed with brine (30 mL x 3), dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give a residue. The residue was purified by flash silica gel chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=92/8 to 83/17) to give (2- formyl-4-phenyl-phenyl) trifluoromethanesulfonate (11.5 g, 34.8 mmol, 98.60% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.35 (s, 1H), 8.20 (d, J = 2.8 Hz, 1H), 7.91 (dd, J = 8.4 ,2.4 Hz, 1H), 7.63-7.62 (m, 1H), 7.60-7.59 (m, 1H), 7.55-7.52 (m, 1H), 7.51 (s, 1H), 7.49 (s, 1H) 7.47-7.43 (m, 1H). [0439] F-1.3 Preparation of 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde [0440] To a solution of (2-formyl-4-phenyl-phenyl) trifluoromethanesulfonate (8 g, 24.2 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2-yl)-1,3,2- dioxaborolane (12.3 g, 48.4 mmol, 2 eq) in dioxane (100 mL) was added Pd(dppf)Cl ₂ -CH ₂ Cl ₂ (989 mg, 1.21 mmol, 0.05 eq), KOAc (4.75 g, 48.4 mmol, 2 eq) at 25°C, the resulting mixture was stirred at 80°C for 5 h. The reaction mixture was filtered, and the filtrate was concentrated in vacuo to give a residue. The residue was purified by flash silica gel chromatography (The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=92/8 to 85/15)) to give 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benz aldehyde (7.4 g, 24.0 mmol, 99.13% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.23 (d, J = 2.0 Hz, 1H), 7.98 (d, J = 7.6 Hz, 1H), 7.84 (dd, J = 8.4, 2.0 Hz, 1H), 7.68-7.67 (m, 1H), 7.66- 7.64 (m, 1H), 7.50-7.46 (m, ₂ H), 7.2-7.40 (m, 1H), 1.42 (s, 1 ₂ H). [0441] F-1.4 Preparation of 1-(1-hydroxy-6-phenyl-2,3,1-benzodiazaborinin-2- yl)ethanone [0442] To a solution of 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (100 mg, 324 umol, 1 eq) and acetohydrazide (24 mg, 324 umol, 1 eq) in EtOH (2 mL) was added NH ₃ .H ₂ O (1.30 mmol, 200 uL, 25% purity, 4.00 eq) dropwise at 25°C, the resulting mixture was stirred at 50°C for 1 h. The mixture was then concentrated in vacuo to give a residue, which was triturated with acetonitrile/H ₂ O (v/v = 3/1, 2 mL) at 25 ^o C for 30 min, then the crude product was triturated with EtOH (2 mL) at 25 ^o C for 30 min. The crude product was triturated with acetonitrile (1.5 mL) at 25 ^o C for 30 min, at last the crude product was triturated with n-pentane (3 mL) at 25 ^o C for 30 min to give 1-(1-hydroxy-6-phenyl-2,3,1- benzodiazaborinin-2-yl) ethanone (21 mg, 74.5 umol, 11.48% yield, 93.70% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.25 (s, 1H), 7.94 (s, 1H), 7.83 (dd, J = 8.0, 2.0 Hz, 1H), 7.75-7.73 (m, 3H), 7.52 (t, J = 7.6 Hz, 2H), 7.41 (t, J = 7.6 Hz, 1H), 2.43 (s, 3H).MS (ESI): mass calcd. For C15H13BN ₂ O2264.11, m/z found 263.1 [M-H]-. HPLC: 93.70% (220 nm), 94.93% (254 nm). [0443] F-2. Preparation of (2-chlorophenyl)-(1-hydroxy-6-phenyl-2,3,1- benzodiazaborinin-2-yl) methanone [0444] To a solution of 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (3.5 g, 11.4 mmol, 1 eq) and 2-chlorobenzohydrazide (1.94 g, 11.4 mmol, 1 eq) in EtOH (30 mL) was added NH ₃ .H ₂ O (3.19 g, 22.7 mmol, 3.5 mL, 25% purity, 2.00 eq) dropwise at 25°C, the resulting mixture was stirred at 70°C for 4 h. The reaction mixture was purified by prep-HPLC directly (column: Agela DuraShell C18250*70mm*10um;mobile phase: [water(10mM NH4H CO3)-ACN]; B%: 15%-43%,22min) to give (2-chlorophenyl) -(1-hydroxy-6- phenyl-2,3,1- benzodiazaborinin-2-yl)methanone (1.18 g, 3.20 mmol, 28.2% yield, 98.05% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.22 (s, 1H), 7.94 (s, 1H),7.90-7.88 (m, 2H), 7.72 (d, J = 7.6 Hz, 2H), 7.62-7.55 (m, 3H), 7.53-7.45 (m, 3H), 7.40 (t, J = 7.2 Hz, 1H). MS (ESI): mass calcd. For C20H14BClN ₂ O2360.08, m/z found 361.2 [M+H] ⁺ . HPLC: 98.05% (220 nm), 99.44% (254 nm). [0445] F-3. Preparation of (1-hydroxy-6-phenyl-2,3,1-benzodiazaborinin-2-yl)-(5- methylthiazol -2-yl)methanone [0446] A mixture of (2-formyl-4-phenyl-phenyl)boronic acid (500 mg, 2.21 mmol, 1 eq) and 5-methylthiazole-2-carbohydrazide (348 mg, 2.21 mmol, 1 eq) in EtOH (10 mL) was added NH ₃ .H ₂ O (1.24 g, 8.85 mmol, 1.4 mL, 25% purity, 4 eq) dropwise, the resulting mixture was stirred at 60°C for 3 h under N ₂ atmosphere. The precipitate was collected by filtration, washed with EtOH (5 mL x 3), dried in vacuo to afford (1-hydroxy-6-phenyl-2,3,1-benzodiazaborinin- 2-yl)-(5-methylthiazol-2-yl)methanone (0.42 g, 1.2 mmol, 54.2% yield) as a yellow solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 7.79-7.77 (m, 1H), 7.74-7.73 (m, 1H), 7.71-7.67 (m, 5H), 7.49 (t, J = 8.0 Hz, ₂ H), 7.38 (t, J = 8.0 Hz, 1H), 2.50 (s, 3H). MS (ESI): mass calcd. For C ₁₈ H ₁₄ BN ₃ O ₂ S 347.09, m/z found 348.1 [M+H] ⁺ . HPLC: 99.29% (220 nm), 99.44% (254 nm). [0447] F-4.1 Preparation of 5-(4-chlorophenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0448] This substance was prepared by following General Procedure F-A. Yellow oil. 1H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.18 (d, J = 1.6 Hz, 1H), 7.97 (d, J = 7.6 Hz, 1H), 7.78 (dd, J = 8.0, 2.0 Hz, 1H), 7.58 (d, J = 8.8 Hz, 2H), 7.43 (d, J = 8.4 Hz, ₂ H), 1.41 (s, 1 ₂ H). [0449] F-4.2 Preparation of (2-chlorophenyl)-[6-(4-chlorophenyl)-1-hydroxy-2,3,1- benzodiazaborinin-2-yl]methanone [0450] This substance was prepared by following General Procedure F-B. White solid, yield: 42.2%. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 8.19 (br s, 1H), 7.90-7.87 (m, ₂ H), 7.80-7.72 (m, 3H), 7.64-7.50 (m, 4H), 7.47-7.30 (m, ₂ H). MS (ESI): mass calcd. For C ₂₀ H ₁₃ BCl ₂ N ₂ O ₂ 394.04, m/z found 395.1 [M+H] ⁺ . HPLC: 96.87% (220 nm), 99.11% (254 nm). [0451] F-5 Preparation of 5-(2-chlorophenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0452] This substance was prepared by following General Procedure F-A. Colorless oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.63 (s, 1H), 8.05 (s, 1H), 7.96 (d, J = 7.6 Hz, 1H), 7.72 (d, J = 7.6 Hz, 1H), 7.51-7.49 (m, 1H), 7.36-7.32 (m, 3H), 1.42 (s, 1 ₂ H). [0453] F-6. Preparation of (2-chlorophenyl)-[6-(2-chlorophenyl)-1-hydroxy-2,3,1 - benzodiazaborinin-2-yl]methanone [0454] This substance was prepared by following General Procedure F-B. White solid, yield: 56.54%. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.21 (s, 1H), 7.88 (d, J = 7.6 Hz, 1H), 7.69 (s, 1H), 7.66 (d, J = 7.6 Hz, 1H), 7.62-7.56 (m, 3H), 7.50 (d, J = 7.2 Hz, 1H), 7.47-7.43 (m, 3H), 7.39-7.35 (m, 1H). MS (ESI): mass calcd. For C ₂₀ H ₁₃ BCl ₂ N ₂ O ₂ 394.04, m/z found 395.0 [M+H] ⁺ . HPLC: 99.27% (220 nm), 98.54% (254 nm). [0455] F-7. Preparation of 1-(1-hydroxy-6-indazol-1-yl-2,3,1-benzodiazaborinin-2- yl)ethenone [0456] F-7.1 Preparation of 1-(4-methoxyphenyl)indazole [0457] To a mixture of 1H-indazole (25 g, 211 mmol, 1 eq) and (4- methoxyphenyl)boronic acid (64.3 g, 423 mmol, 2 eq) in DCM (600 mL) was added Et ₃ N (423 mmol, 58.9 mL, 2 eq) and Cu(OAc) ₂ (38.4 g, 211 mmol, 1 eq) in one portion at 20°C under O ₂ atmosphere, the resulting mixture was stirred at 35°C for 80 h. The mixture was poured into ice-water (w/w = 1/1) (1000 mL), the pH of the aqueous phase was adjusted to 5-6 with HCl (2N), and the aqueous phase was extracted with DCM (300 mL x 2). The combined organic phase was washed with brine (200 mL), dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give a residue, which was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 1-(4-methoxyphenyl)indazole (15 g, 66.8 mmol, 31.6% yield) as a yellow oil. ¹ H NMR (CDCl _3, 400 MHz) δ 8.19 (s, 1H), 8.81 (d, J = 8.4 Hz, 1H), 7.67 (d, J = 8.8 Hz, 1H), 7.63 (d, J = 9.2 Hz, 2H), 7.42 (t, J = 7.2 Hz, 1H), 7.22 (t, J = 7.2 Hz, 1H), 7.07 (d, J = 8.8 Hz, ₂ H), 3.89 (s, 3H). [0458] F-7.2 Preparation of 4-indazol-1-ylphenol [0459] To a mixture of 1-(4-methoxyphenyl)indazole (15 g, 66.9 mmol, 1 eq) in DCM (150 mL) was added BBr ₃ (200 mmol, 19.3 mL, 3 eq) dropwise at 0°C, the resulting mixture was stirred at 25°C for 16 h. The mixture was poured into ice-water (w/w = 1/1) (200 mL) and sat.aq.NaHCO ₃ (50 mL ), the aqueous phase was extracted with DCM (50 mL x 2). The combined organic phase was washed with brine (30 mL), dried over anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuo to give a residue, which was triturated with MTBE (50 mL) to give 4- indazol-1-ylphenol (13 g, 61.8 mmol, 92.4% yield) as an off-white solid. ¹ H NMR (DMSO-d _6, 400 MHz) δ 8.29 (s, 1H), 8.86 (d, J = 8.4 Hz, 1H), 7.67 (d, J = 8.4 Hz, 1H), 7.51 (d, J = 6.8 Hz, 2H), 7.44 (t, J = 8.0 Hz, 1H), 7.22 (t, J = 7.2 Hz, 1H), 6.96 (d, J = 6.4 Hz, ₂ H). [0460] F-7.3 Preparation of 2-hydroxy-5-indazol-1-yl-benzaldehyde [0461] To a mixture of 4-indazol-1-ylphenol (13 g, 61.8 mmol, 1 eq) and (HCHO) _n (18.6 g, 618 mmol, 10 eq) in THF (300 mL) was added MgCl ₂ (9.56 g, 100 mmol, 1.62 eq) and Et ₃ N (247 mmol, 34.4 mL, 4 eq) in one portion at 20°C under N ₂ atmosphere, the resulting mixture was heated to 80°C and stirred for 16 h. The reaction mixture was poured into ice-water (w/w = 1/1) (500 mL), and pH of the aqueous phase was adjusted to 4-5 with HCl (2N), the resulting mixture was filtered. The filtrate was extracted with ethyl acetate (200 mL x 3), and the combined organic phase was washed with brine (200 mL x 2), dried over anhydrous Na2SO4, filtered and concentrated in vacuo to give a residue, which was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=1/0 to 10/1) to give 2-hydroxy-5-indazol- 1-yl-benzaldehyde (6 g, 25.2 mmol, 40.7% yield) as a yellow solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 11.04 (s, 1H), 10.36 (s, 1H), 8.36 (s, 1H), 7.93-7.90 (m, ₂ H), 7.89 (d, J = 8.4 Hz, 1H), 7.73 (d, J = 8.4 Hz, 1H), 7.49 (t, J = 8.0 Hz, 1H), 7.28-7.21 (m, ₂ H). [0462] F-7.4 Preparation of (2-formyl-4-indazol-1-yl-phenyl) trifluoromethanesulfonate [0463] To a mixture of 2-hydroxy-5-indazol-1-yl-benzaldehyde (6 g, 25.2 mmol, 1 eq) and Et3N (75.6 mmol, 10.5 mL, 3 eq) in DCM (60 mL) was added Tf ₂ O (30.2 mmol, 4.99 mL, 1.2 eq) dropwise at 0°C, the resulting mixture was stirred at 20°C for 2 h. The reaction was then quenched by adding sat. aq. NH4Cl (120 mL) at 0°C, the aqueous phase was extracted with DCM (60 mL x 2). The combined organic phase was washed with brine (50 mL), dried over anhydrous Na2SO4, filtered and concentrated in vacuo to give a residue, which was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=10/1 to 5/1) to give (2-formyl-4- indazol-1-yl-phenyl) trifluoromethanesulfonate (8 g, 21.6 mmol, 85.8% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.36 (s, 1H), 8.41 (d, J = 3.2 Hz, 1H), 8.27 (s, 1H), 8.18 (dd, J = 8.8, 2.8 Hz, 1H), 7.84 (t, J = 9.2 Hz, 2H), 7.61 (d, J = 8.8 Hz, 1H), 7.54 (t, J = 8.4 Hz, 1H), 7.32 (t, J = 7.2 Hz, 1H). [0464] F-7.5 Preparation of 5-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan- 2-yl) benzaldehyde [0465] To a mixture of (2-formyl-4-indazol-1-yl-phenyl) trifluoromethanesulfonate (8 g, 21.6 mmol, 1 eq) and 4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane) (13.7 g, 54.0 mmol, 2.5 eq) in dioxane (120 mL) was added KOAc (5.30 g, 54.0 mmol, 2.5 eq) and Pd(dppf)Cl ₂ (0.948 g, 1.30 mmol, 0.06 eq) in one portion at 25°C under N ₂ atmosphere, the resulting mixture was heated to 80°C and stirred for 16 h. The reaction mixture was filtered and concentrated in vacuo to give a residue, which was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 5-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan -2-yl)benzaldehyde (8 g, crude) as a white solid. ¹ H NMR (CDCl _3, 400 MHz) δ 10.73 (s, 1H), 8.40 (s, 1H), 8.24 (s, 1H), 8.11-8.08 (m, 1H), 8.07-8.03 (m, 1H), 7.86-7.80 (m, 2H), 7.49 (t, J = 6.8 Hz, 1H), 7.27 (t, J = 7.6 Hz, 1H), 1.43 (s, 12H). [0466] F-7.6 Preparation of 1-(1-hydroxy-6-indazol-1-yl-2,3,1-benzodiazaborinin-2- yl)ethanone [0467] To a mixture of 5-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (300 mg, 861 umol, 1 eq) in EtOH (3 mL) was added acetohydrazide (64 mg, 861 umol, 1 eq) and NH ₃ .H ₂ O (1.95 mmol, 0.3 mL, 25% purity, 2.26 eq) in one portion at 20°C under N ₂ atmosphere, the resulting mixture was heated to 50°C and stirred for 2 h. The reaction mixture was concentrated in vacuo to give a residue, which was purified by prep-HPLC (column: Waters Xbridge Prep OBD C18150*40mm*10um; mobile phase: [water(0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 10%-50%,7min) to give 1-(1-hydroxy-6- indazol-1-yl-2,3,1-benzodiazaborinin-2-yl)ethanone (100 mg, 326 umol, 37.9% yield, 99.3% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.44 (s, 1H), 8.37 (s, 1H), 8.09 (s, 1H), 8.00 (d, J = 8.4 Hz, 1H), 7.98-7.92 (m, ₂ H), 7.86 (d, J = 7.6 Hz, 1H), 7.55 (t, J = 7.6 Hz, 1H), 7.31 (t, J = 7.6 Hz, 1H), 2.47 (s, 3H). MS (ESI): mass calcd. For C16H13BN4O2304.11, m/z found 305.2 [M+H] ⁺ . HPLC: 99.26% (220 nm), 99.23% (254 nm). [0468] F-8. Preparation of 5-(3-fluorophenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0469] This substance was prepared by following General Procedure F-A. Yellow solid. 1H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.20 (d, J = 2.0 Hz, 1H), 7.98 (d, J = 8.0 Hz, 1H), 7.81 (dd, J = 8.0, 2.0 Hz, 1H), 7.45-7.43 (m, ₂ H), 7.37-7.34 (m, 1H), 7.13-7.07 (m, 1H), 1.42 (s, 12H). [0470] F-9. Preparation of (2-chlorophenyl)-[6-(3-fluorophenyl)-1-hydroxy-2,3,1- benzodiazabor inin-2-yl]methanone [0471] This substance was prepared by following General Procedure F-B. White solid. 1H NMR (DMSO-d6, 400 MHz) δ 8.21 (s, 1H), 8.00 (s, 1H), 7.94 (d, J = 7.6 Hz, 1H), 7.88 (d, J = 8.0 Hz, 1H), 7.63-7.47 (m, 8H), 7.27-7.22 (m, 1H). MS (ESI): mass calcd. For C20H13BClFN ₂ O2 378.07, m/z found 379.1 [M+H] ⁺ . HPLC: 99.35% (220 nm), 99.58% (254 nm). [0472] F-10. Preparation of 1-[7-(3,4-dimethoxyphenyl)-1-hydroxy-2,3,1- benzodiazaborinin-2- yl]ethanone [0473] F10.1 Preparation of (4-formyl-3-hydroxy-phenyl) trifluoromethanesulfonate [0474] To a solution of 2,4-dihydroxybenzaldehyde (20 g, 144.80 mmol, 1 eq) in DCM (200 mL) was added pyridine (11.45 g, 144.80 mmol, 11.69 mL, 1 eq), then Tf ₂ O (40.85 g, 144.80 mmol, 23.89 mL, 1 eq) was added to the mixture drop-wise at 0°C. The reaction mixture was warmed to 25°C and stirred for 12 h. The reaction mixture was quenched by addition ice:H ₂ O (v:v=1:1, 150 mL), and then extracted with DCM (100 mL x 3). The combined organic layers were washed with brine (100 mL x 2), dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~11% Ethyl acetate/Petroleum ethergradient @ 200 mL/min) to give (4-formyl-3-hydroxy-phenyl) trifluoromethanesulfonate (5.3 g, 19.62 mmol, 13.55% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.30 (s, 1H), 9.94 (s, 1H), 7.69 (d, J = 8.8Hz, 1H), 6.97-6.94 (m, ₂ H). [0475] F10.2 Preparation of 4-(3,4-dimethoxyphenyl)-2-hydroxy-benzaldehyde [0476] To a mixture of (4-formyl-3-hydroxy-phenyl) trifluoromethanesulfonate (5.3 g, 19.62 mmol, 1 eq) in DME (60 mL) was added TPP (121mg, 196.16 umol, 0.01 eq), Pd(OAc)2 (0.044 g, 196.16 umol, 0.01 eq), K ₂ CO ₃ (8.13 g, 58.85 mmol, 3 eq) and (3,4- dimethoxyphenyl)boronic acid (4.28 g, 23.54 mmol, 1.2 eq) in one portion at 25°C. The mixture was stirred at 25°C for 12 h. The reaction mixture was filtered with celite and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~29% Ethyl acetate/Petroleum ethergradient @ 200 mL/min) to give 4-(3,4-dimethoxyphenyl)-2-hydroxy- benzaldehyde (1.05 g, 4.07 mmol, 20.73% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.16 (s, 1H), 9.92 (s, 1H), 7.60 (d, J = 8.0 Hz, 1H), 7.26-7.25 (m, 1H), 7.24-7.23 (m, 1H), 7.20 (s, 1H), 7.15 (d, J = 2.0 Hz, 1H), 6.98 (d, J = 8.4Hz, 1H), 3.97 (s, 3H), 3.95 (s, 3H). [0477] F10.3 Preparation of [5-(3,4-dimethoxyphenyl)-2-formyl-phenyl] trifluoromethanesulfonate [0478] To a mixture of 4-(3,4-dimethoxyphenyl)-2-hydroxy-benzaldehyde (850 mg, 3.29 mmol, 1 eq) in DCM (10 mL) was added TEA (999 mg, 9.87 mmol, 1.37 mL, 3 eq) and DMAP (8 mg, 65.82 umol, 0.02 eq) in one portion at 0°C, then 1,1,1-trifluoro-N-phenyl-N- (trifluoromethylsulfonyl)methanesulfonamide (1.76 g, 4.94 mmol, 1.5 eq) was added to the mixture at 0°C. The mixture was stirred at 25°C for 4 h. The reaction mixture was concentrated under reduced pressure. The residue was purified by flash silica gel chromatography (ISCO®; 20 g SepaFlash® Silica Flash Column, Eluent of 0~26% Ethyl acetate/Petroleum ethergradient @ 200 mL/min) to give [5-(3,4-dimethoxyphenyl) -2-formyl-phenyl] trifluoromethanesulfonate (1.05 g, 2.69 mmol, 81.74% yield) as a yellow solid. [0479] F10.4 Preparation of 4-(3,4-dimethoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0480] To a mixture of [5-(3,4-dimethoxyphenyl)-2-formyl-phenyl] trifluoromethanesulfonate (1 g, 2.56 mmol, 1 eq) in dioxane (20 mL) was added BPD (0.8 g, 3.07 mmol, 1.2 eq), KOAc (503 mg, 5.12 mmol, 2 eq) and Pd(dppf)Cl ₂ (0.19 mg, 256.19 umol, 0.1 eq) in one portion at 25°C under N ₂ . The mixture was heated to 80°C and stirred for 6 h. The reaction mixture was filtered with celite and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 20 g SepaFlash® Silica Flash Column, Eluent of 0~34% Ethyl acetate/Petroleum ethergradient @ 200 mL/min) to give 4-(3,4-dimethoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxabo rolan-2-yl)benzaldehyde (1 g, 2.72 mmol, yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.56 (s, 1H), 8.03 (d, J = 8.0 Hz, ₂ H), 7.74 (d, J = 8.0 Hz, 1H), 7.25 (d, J = 2.0 Hz, 1H), 7.16 (d, J =2.4 Hz, 1H), 6.98 (d, J = 8.4 Hz, 1H), 3.98 (s, 3H), 3.95 (s, 3H), 1.43 (s, 1 ₂ H). [0481] F10.5 Preparation of 1-[7-(3,4-dimethoxyphenyl)-1-hydroxy-2,3,1- benzodiazaborinin-2- yl]ethanone [0482] To a solution of 4-(3,4-dimethoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde (250 mg, 678.92 umol, 1 eq) in EtOH (3 mL) was added acetohydrazide (55 mg, 746.82 umol, 1.1 eq) and NH ₃ .H ₂ O (273 mg, 1.95 mmol, 0.3 mL, 25% purity, 2.87 eq) at 25°C, the mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated under reduced pressure to give a residue. The residue was purified by prep- HPLC (column: Welch Xtimate C18150*25mm*5um;mobile phase: [water (0.05% ammonia hydroxide v/v)-ACN];B%: 5%-45%,10.5min) to give 1-[7-(3,4-dimethoxyphenyl)-1-hydroxy-2,3,1- benzodiazaborinin -2-yl]ethanone (66 mg, 194.90 umol, 28.71% yield, 95.72% purity) as an off- white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.17 (s, 1H), 7.85 (s, 1H), 7.79 (dd, J = 1.6, 8.0 Hz, 1H), 7.66 (d, J = 8.0 Hz, 1H), 7.23-7.23 (m, ₂ H), 7.01 (d, J = 8.0 Hz, 1H), 3.82 (s, 3H), 3.77 (s, 3H), 2.43 (s, 3H). MS (ESI): mass calcd. For C17H17BN ₂ O4, 324.13, m/z found 325.2 [M+H] ⁺ . HPLC: 95.72% (220 nm), 92.13 (254 nm). [0483] F-11 Preparation of 3-hydroxy-1-(1-hydroxy-6-phenyl-2,3,1- benzodiazaborinin-2-yl) -4-methyl-pentan-1-one

[0484] F11.1 Preparation of 2-hydroxy-5-phenyl-benzaldehyde [0485] To a mixture of 5-bromo-2-hydroxy-benzaldehyde (10 g, 49.8 mmol, 1 eq) and phenylboronic acid (9.10 g, 74.6 mmol, 1.5 eq) in H ₂ O (350 mL) was added K ₂ CO ₃ (13.8 g, 99.5 mmol, 2 eq) and palladium;triphenylphosphane (0.144 g, 124 umol, 0.0025 eq) at 25°C under N ₂ . The resulting suspension was stirred at 80°C for 6 h. The reaction mixture was cooled and then the precipitate formed, the precipitate was collected and washed with water (50 mL) to give 2-hydroxy-5-phenyl-benzaldehyde (8.3 g, 40.6 mmol, 81.65% yield, 97% purity) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.01 (s, 1H), 10.00 (s, 1H), 7.80-7.78 (m, 2H), 7.58-7.56 (m, 2H), 7.47 (t, J = 7.6 Hz, ₂ H), 7.37 (t, J = 7.2 Hz,, 1H), 7.10 (d, J = 8.4 Hz, 1H). [0486] F11.2 Preparation of (2-formyl-4-phenyl-phenyl) trifluoromethanesulfonate -142- [0487] To a mixture of 2-hydroxy-5-phenyl-benzaldehyde (7 g, 35.3 mmol, 1 eq) and pyridine (106 mmol, 8.55 mL, 3 eq) in DCM (100 mL) was added Tf ₂ O (53.0 mmol, 8.74 mL, 1.5 eq) dropwise at 0°C, the mixture was stirred at 0°C for 2 h. The reaction mixture was poured into sat.aq NH4Cl (150 mL), and extracted with DCM (80 mL x 3). The combined organic layers were washed with brine (30 mL x 3), dried over Na2SO4, filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (SiO2, Petroleum ether/Ethyl acetate=92/8 to 83/17) to give (2-formyl-4-phenyl-phenyl) trifluoromethanesulfonate (11.5 g, 34.8 mmol, 98.60% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.35 (s, 1H), 8.20 (d, J = 2.8 Hz, 1H), 7.91 (dd, J = 8.4 ,2.4 Hz, 1H), 7.63-7.62 (m, 1H), 7.60-7.59 (m, 1H), 7.55-7.52 (m, 1H), 7.51 (s, 1H), 7.49 (s, 1H) 7.47-7.43 (m, 1H). [0488] F-11.3 Preparation of 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde [0489] To a solution of (2-formyl-4-phenyl-phenyl) trifluoromethanesulfonate (8 g, 24.2 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2-yl)-1,3,2- dioxaborolane (12.3 g, 48.4 mmol, 2 eq) in dioxane (100 mL) was added Pd(dppf)Cl ₂ .CH ₂ Cl ₂ (989 mg, 1.21 mmol, 0.05 eq), KOAc (4.75 g, 48.4 mmol, 2 eq) at 25°C, the mixture was stirred at 80°C for 5 h. The reaction mixture was filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=92/8 to 85/15)) to give 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benz aldehyde (7.4 g, 24.0 mmol, 99.13% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.23 (d, J = 2.0 Hz, 1H), 7.98 (d, J = 7.6 Hz, 1H), 7.84 (dd, J = 8.4, 2.0 Hz, 1H), 7.68-7.67 (m, 1H), 7.66-7.64 (m, 1H), 7.50-7.46 (m, ₂ H), 7.2-7.40 (m, 1H), 1.42 (s, 12H). [0490] F-11.4 Preparation of methyl 3-hydroxy-4-methylpentanoate [0491] To a solution of methyl 4-methyl-3-oxo-pentanoate (2.07 g, 12.64 mmol, 2.04 mL, 1 eq) in THF (20 mL) and MeOH (1 mL) was added NaBH ₄ (957 mg, 25.29 mmol, 2 eq) at 0°C, the mixture was stirred at 0 °C for 1 h. The reaction mixture was quenched with H ₂ O (5 mL) and concentrated in vacuo. The residue was diluted with EtOAc (100 mL) and the organic layer was washed with H ₂ O (30 mL x 2). The organic layer was washed with brine, dried over Na ₂ SO ₄ , filtered and concentrated in vacuo to give the product methyl 3-hydroxy-4-methyl-pentanoate (2 g, crude), which was used into the next step without further purification. [0492] F-11.5 Preparation of methyl 3-hydroxy-4-methylpentanehydrazide [0493] To a solution of methyl 3-hydroxy-4-methyl-pentanoate (2.0 g, 13.68 mmol, 1 eq) in EtOH (20 mL) was added NH ₂ NH ₂ .H ₂ O (2.05 g, 41.04 mmol, 1.99 mL, 3 eq). The mixture was stirred at 90°C for 12 h. The reaction mixture was cooled to 25 ^o C and concentrated in vacuo to give the product 3-hydroxy-4-methyl-pentanehydrazide (2 g, crude) as a white solid, which was used in the next step without further purification. [0494] F11.6 Preparation of 3-hydroxy-1-(1-hydroxy-6-phenyl-2,3,1- benzodiazaborinin-2-yl) -4-methyl-pentan-1-one [0495] To a solution of 5-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (100 mg, 324 umol, 1 eq) and 3-hydroxy-4-methyl-pentanehydrazide (47 mg, 324 umol, 1 eq) in EtOH (3 mL) was added NH ₃ .H ₂ O (0.1 mL, 649 umol, 25% purity, 2.00 eq) drop-wise at 25°C, the mixture was stirred at 50°C for 1 h. The reaction mixture was concentrated in vacuum. The residue was purified by prep-HPLC (column: Welch Xtimate C18 150*25mm*5um;mobile phase: [water (0.05% ammonia hydroxide v/v)-ACN];B%: 10%- 40%,10.5min) to give 3-hydroxy-1-(1-hydroxy-6-phenyl-2,3,1-benzodiazaborinin-2-yl )-4- methyl-pentan-1-one (11 mg, 30 umol, 9.39% yield, 93.13% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) 8.35-8.31 (m, 1H), 8.16-8.14 (m, 1H), 8.10-8.06 (m, 1H), 8.03-8.00 (m, 1H), 7.82-7.81 (m, 1H), 7.81-7.79 (m, 1H), 7.54 (t, J = 7.6 Hz, ₂ H), 7.47-7.42 (m, 1H), 4.31-4.21 (m, 1H), 2.92-2.73 (m, ₂ H), 1.97-1.81 (s, 1H), 1.04 (d, J = 6.8 Hz, 3H), 0.99 (d, J = 6.8 Hz, 3H). MS (ESI): mass calcd. For C19H21BN ₂ O3336.16, m/z found 319.0 [M+H-18] ⁺ . HPLC: 93.13% (220 nm), 95.17% (254 nm). [0496] F12 Preparation of 1-(1-hydroxy-7-phenyl-2,3,1-benzodiazaborinin-2- yl)ethanone [0497] F12.1 Preparation of 2-hydroxy-4-phenyl-benzaldehyde [0498] To a mixture of 4-bromo-2-hydroxy-benzaldehyde (5 g, 24.8 mmol, 1 eq) and phenylboronic acid (3.94 g, 32.3 mmol, 1.3 eq) in toluene (60 mL) and H ₂ O (10 mL) was added Pd(PPh3)4 (1.44 g, 1.24 mmol, 0.05 eq), K ₂ CO ₃ (6.88 g, 49.7 mmol, 2 eq) in one portion at 20°C under N ₂ . The mixture was heated to 90°C and stirred for 4 h. The mixture was poured into ice- water (w/w = 1/1) (100 mL) and stirred for 2 min. The aqueous phase was extracted with ethyl acetate (50 mL x 3), the combined organic phase was washed with brine (50 mL x 2), dried with anhydrous Na2SO4, filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=20/1 to 10/1) to give 2-hydroxy-4- phenyl-benzaldehyde (4.4 g, 22.2 mmol, 89.2% yield) as an off-white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.11 (s, 1H), 9.91 (s, 1H), 7.63-7.59 (m, 3H), 7.47-7.44 (m, 3H), 7.25-7.20 (m, 2H). [0499] F12.2 Preparation of (2-formyl-5-phenyl-phenyl) trifluoromethanesulfonate [0500] To a mixture of 2-hydroxy-4-phenyl-benzaldehyde (4 g, 20.2 mmol, 1 eq) in DCM (50 mL) was added pyridine (4.79 g, 60.5 mmol, 4.89 mL, 3 eq) at 0°C, then Tf ₂ O (24.2 mmol, 4 mL, 1.2 eq) was added to the mixture at 0°C. The resulting mixture was stirred at 20°C for 1 h. The reaction mixture was quenched by addition sat.aq.NH ₄ Cl (100 mL) at 0°C, and extracted with DCM (50 mL x 2), the combined organic phase was washed with brine (50 mL ), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=20/1 to 10/1) to give (2-formyl-5-phenyl- phenyl) trifluoromethanesulfonate (6 g, 18.1 mmol, 90.0% yield) as a yellow solid. ¹ H NMR (CDCl _3, 400 MHz) δ 10.31 (s, 1H), 8.07 (d, J = 8.4 Hz, 1H), 7.78 (d, J = 8.0 Hz, 1H), 7.64-7.60 (m, 3H), 7.53-7.47 (m, 3H). [0501] F12.3 Preparation of 4-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde [0502] To a mixture of (2-formyl-5-phenyl-phenyl) trifluoromethanesulfonate (3 g, 9.08 mmol, 1 eq) in dioxane (50 mL) was added Pd(dppf)Cl ₂ (0.400 g, 546 umol, 6.02e-2 eq), KOAc (1.69 g, 17.2 mmol, 1.9 eq) and 4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane) (2.63 g, 10.4 mmol, 1.14 eq) in one portion at 25°C under N ₂ , then the mixture was heated to 80°C and stirred for 16 h. The reaction mixture was filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=10/1 to 5/1). The crude product was triturated with Petroleum ether (20 mL) at 25 ^o C for 30 min to give 4-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benz aldehyde (0.7 g, 2.26 mmol, 24.9% yield, 99.5% purity) as a white solid. ¹ H NMR (DMSO-d _6, 400 MHz) δ 10.37 (s, 1H), 8.00 (d, J = 8.4 Hz, 1H), 7.96-7.93 (m, 2H), 7.74 (d, J = 7.2 Hz, 2H), 7.52 (t, J = 7.2 Hz, ₂ H), 7.45 (t, J = 7.6 Hz, 1H), 1.37 (s, 12H). MS (ESI): mass calcd. For C ₁₉ H ₂₁ BO ₃ 308.16, m/z found 309.1 [M+H] ⁺ . HPLC: 99.45% (220 nm), 99.41% (254 nm). [0503] F12.4 Preparation of 1-(1-hydroxy-7-phenyl-2,3,1-benzodiazaborinin-2- yl)ethanone [0504] To a mixture of 4-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (400 mg, 1.30 mmol, 1 eq) in EtOH (6 mL) was added acetohydrazide (100 mg, 1.35 mmol, 1.04 eq) and NH ₃ .H ₂ O (1.30 mmol, 0.2 mL, 25% purity, 1 eq) in one portion at 20°C under N ₂ . The mixture was heated to 50°C and stirred for 2 h. The reaction mixture was concentrated under reduced pressure to give a residue. The residue was purified by prep- HPLC (column: Welch Xtimate C18150*25mm*5um;mobile phase: [water (0.05% ammonia hydroxide v/v)-ACN];B%: 5%-40%,10.5min) to give 1-(1-hydroxy-7-phenyl-2,3,1- benzodiazaborinin-2-yl) ethanone (75 mg, 268 umol, 20.7% yield, 94.5% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.20 (s, 1H), 7.89 (s, 1H), 7.81 (dd, J = 8.4, 2.0 Hz, 1H), 7.72-7.69 (m, 3H), 7.45 (t, J = 7.2 Hz, 2H), 7.37 (t, J = 6.8 Hz, 1H), 2.43 (s, 3H). MS (ESI): mass calcd. For C ₁₅ H ₁₃ BN ₂ O ₂ 264.11, m/z found 265.1 [M+H] ⁺ . HPLC: 94.47% (220 nm), 93.81% (254 nm). [0505] F13 Preparation of 1-(1-hydroxy-7-indazol-1-yl-2,3,1-benzodiazaborinin-2- yl)ethanone [0507] A mixture of 1H-indazole (2.50 g, 21 mmol, 1 eq), Cs ₂ CO ₃ (6.90 g, 21 mmol, 1 eq) in DMSO (50 mL) was stirred at 130°C for 10 min, and then 2-bromo-4-fluoro-benzaldehyde (4.73 g, 23.28 mmol, 1.1 eq) was added in portions at 130°C. The result mixture was stirred at 130°C for additional 2 h. The reaction mixture was partitioned between Ethyl acetate (100 mL) and Sat.NH ₄ Cl (100 mL). The organic phase was separated, washed with brine (50 mL x 2), dried over Na ₂ SO ₄ , filtered and concentrated under reduced pressure to give a residue. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=1/0 to 3/1) to give 2-bromo-4-indazol-1-yl-benzaldehyde (4.31 g, 14 mmol, 34% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.38 (s, 1H), 8.28 (s, 1H), 8.17 (d, J = 2.4 Hz, 1H), 8.13 (d, J = 8.8 Hz, 1H), 7.92 (dd, J = 8.4 Hz, J = 1.6 Hz, 1H), 7.86 (m, ₂ H), 7.55 (d, J = 8.0 Hz, 1H), 7.33 (d, J = 8.0 Hz, 1H). [0508] F13.2 Preparation of 4-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan -2-yl)benzaldehyde [0509] A mixture of 2-bromo-4-indazol-1-yl-benzaldehyde (2.50 g, 8 mmol, 1 eq), 4,4, 4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane) (21.1 g, 83 mmol, 10 eq), KOAc (2.44 g, 25 mmol, 3 eq) and Pd(dppf)Cl ₂ (607 mg, 830 umol, 0.1 eq) in dioxane (50 mL) was degassed and purged with N ₂ for 3 times, and then the mixture was stirred at 90°C for 16 h under N ₂ atmosphere. The reaction mixture was partitioned between Ethyl acetate (100 mL) and H ₂ O (50 mL). The organic phase was separated, washed with brine (50 mL mL x 2), dried over Na ₂ SO ₄ , filtered and concentrated under reduced pressure to give a residue. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=1/0 to 3/1) to give 4-indazol-1- yl-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan -2-yl)benzaldehyde (770 mg, 2 mmol, 27% yield) as a white solid. 190 mg of crude product (from 770 mg) was triturated with Petroleum ether to give 4-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan -2-yl) benzaldehyde (33 mg, 96.96% purity) as a white solid. ¹ H NMR (DMSO, 400 MHz) δ 10.40 (s, 1H), 8.52 (s, 1H), 8.15 (s, 3H), 8.00 (d, J = 8.0 Hz, 1H), 7.96 (t, J = 8.0 Hz, 1H), 7.60 (t, J = 7.6 Hz, 1H), 7.36 (t, J = 7.2 Hz, 1H), 1.39 (s, 12H). MS (ESI): mass calcd. For C ₂₀ H ₂₁ BN ₂ O ₃ 348.16, m/z found 267.0 [M- 82+H] ⁺ . HPLC: 96.96% (220 nm), 97.64% (254 nm). [0510] F13.3 Preparation of 1-(1-hydroxy-7-indazol-1-yl-2,3,1-benzodiazaborinin-2- yl)ethanone [0511] A mixture of 4-indazol-1-yl-2-(4,4,6,6-tetramethyl-1,3,2-dioxaborinan-2- yl)benzaldehyde (190 mg, 525 umol, 1 eq), acetohydrazide (39 mg, 525 umol, 1 eq) and NH ₃ .H ₂ O (31 mg, 2 mmol, 25% purity, 3 eq) in EtOH (2 mL) was stirred at 50°C for 1 h. The reaction mixture was filtered. The filtrate was purified by reversed-phase HPLC (column: Phenomenex Gemini-NX C1875*30mm*3um;mobile phase: [water(10mM NH ₄ HCO ₃ )-ACN]; B%: 5%-40%,10.5min) to give 1-(1-hydroxy-7-indazol-1-yl-2,3,1-benzodiazaborinin-2-yl) ethanone (24 mg, 79 umol, 15% yield) as a white solid. ¹ H NMR (DMSO, 400 MHz) δ 8.40-8.28 (m, 1H), 8.01-7.84 (m, 4H), 7.54 - 7.50 (m, 3H), 7.28 (t, J = 7.6 Hz, 1H), 2.46 (s, 1H), 2.26-2.13 (m, 2H). MS (ESI): mass calcd. For C ₁₆ H ₁₃ BN ₄ O ₂ 304.11, m/z found 305.2 [M+H] ⁺ . HPLC: 98.95% (220 nm), 99.39% (254 nm). [0512] F14 Preparation of (1-hydroxy-6- indazol-1-yl-2,3,1-benzodiazaborinin-2-yl)- (5-methylthiazol-2-yl)methanone [0514] To a mixture of 1H-indazole (25 g, 211 mmol, 1 eq) and (4- methoxyphenyl)boronic acid (64.3 g, 423 mmol, 2 eq) in DCM (600 mL) was added Et3N (423 mmol, 58.9 mL, 2 eq) and Cu(OAc)2 (38.4 g, 211 mmol, 1 eq) in one portion at 20°C under O2. The mixture was stirred at 35°C for 80 h. The mixture was poured into ice-water (w/w = 1/1) (1000 mL) and the aqueous phase was adjusted pH to 5-6 with HCl (2N), the aqueous phase was extracted with DCM (300 mL x 2), the combined organic phase was washed with brine (200 mL), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 1- (4-methoxyphenyl)indazole (15 g, 66.8 mmol, 31.6% yield) as a yellow oil. ¹ H NMR (CDCl _3, 400 MHz) δ 8.19 (s, 1H), 8.81 (d, J = 8.4 Hz, 1H), 7.67 (d, J = 8.8 Hz, 1H), 7.63 (d, J = 9.2 Hz, 2H), 7.42 (t, J = 7.2 Hz, 1H), 7.22 (t, J = 7.2 Hz, 1H), 7.07 (d, J = 8.8 Hz, ₂ H), 3.89 (s, 3H). [0515] F14.2 Preparation of 4-indazol-1-ylphenol [0516] To a mixture of 1-(4-methoxyphenyl)indazole (15 g, 66.9 mmol, 1 eq) in DCM (150 mL) was added BBr ₃ (200 mmol, 19.3 mL, 3 eq) drop-wise at 0°C. The mixture was stirred at 25°C for 16 h. The mixture was poured into ice-water (w/w = 1/1) (200 mL) and sat.aq.NaHCO ₃ (50 mL ), the aqueous phase was extracted with DCM (50 mL x 2), the combined organic phase was washed with brine (30 mL), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The crude product was triturated with MTBE (50 mL) at 20 ^o C for 20 min to give 4-indazol-1-ylphenol (13 g, 61.8 mmol, 92.4% yield) as an off-white solid. ¹ H NMR (DMSO-d _6, 400 MHz) δ 8.29 (s, 1H), 8.86 (d, J = 8.4 Hz, 1H), 7.67 (d, J = 8.4 Hz, 1H), 7.51 (d, J = 6.8 Hz, 2H), 7.44 (t, J = 8.0 Hz, 1H), 7.22 (t, J = 7.2 Hz, 1H), 6.96 (d, J = 6.4 Hz, 2H). [0517] F14.3 Preparation of 2-hydroxy-5-indazol-1-yl-benzaldehyde [0518] To a mixture of 4-indazol-1-ylphenol (13 g, 61.8 mmol, 1 eq) and (HCHO) _n (18.6 g, 618 mmol, 10 eq) in THF (300 mL) was added MgCl ₂ (9.56 g, 100 mmol, 1.62 eq) and Et ₃ N (247 mmol, 34.4 mL, 4 eq) in one portion at 20°C under N ₂ . The mixture was heated to 80°C and stirred for 16 h. The reaction mixture was poured into ice-water (w/w = 1/1) (500 mL) and the aqueous phase was adjusted pH to 4-5 with HCl (2N), the mixture was filtered and the filtrate was extracted with ethyl acetate (200 mL x 3), the combined organic phase was washed with brine (200 mL x 2), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=1/0 to 10/1) to give 2-hydroxy-5-indazol-1-yl-benzaldehyde (6 g, 25.2 mmol, 40.7% yield) as a yellow solid. ¹ H NMR (DMSO-d _6, 400 MHz) δ 11.04 (s, 1H), 10.36 (s, 1H), 8.36 (s, 1H), 7.93- 7.90 (m, 2H), 7.89 (d, J = 8.4 Hz, 1H), 7.73 (d, J = 8.4 Hz, 1H), 7.49 (t, J = 8.0 Hz, 1H), 7.28- 7.21 (m, 2H). [0519] F14.4 Preparation of (2-formyl-4-indazol-1-yl-phenyl) trifluoromethanesulfonate [0520] To a mixture of 2-hydroxy-5-indazol-1-yl-benzaldehyde (6 g, 25.2 mmol, 1 eq) and Et3N (75.6 mmol, 10.5 mL, 3 eq) in DCM (60 mL) was added Tf ₂ O (30.2 mmol, 4.99 mL, 1.2 eq) drop-wise at 0°C. The mixture was stirred at 20°C for 2 h. The reaction mixture was quenched by addition sat.aq.NH4Cl (120 mL) at 0°C, and extracted with DCM (60 mL x 2), the combined organic phase was washed with brine (50 mL), dried with anhydrous Na2SO4, filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=10/1 to 5/1) to give (2-formyl-4-indazol-1-yl-phenyl) trifluoromethanesulfonate (8 g, 21.6 mmol, 85.8% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.36 (s, 1H), 8.41 (d, J = 3.2 Hz, 1H), 8.27 (s, 1H), 8.18 (dd, J = 8.8, 2.8 Hz, 1H), 7.84 (t, J = 9.2 Hz, ₂ H), 7.61 (d, J = 8.8 Hz, 1H), 7.54 (t, J = 8.4 Hz, 1H), 7.32 (t, J = 7.2 Hz, 1H). [0521] F14.5 Preparation of 5-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0522] To a mixture of (2-formyl-4-indazol-1-yl-phenyl) trifluoromethanesulfonate (8 g, 21.6 mmol, 1 eq) and 4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane) (13.7 g, 54.0 mmol, 2.5 eq) in dioxane (120 mL) was added KOAc (5.30 g, 54.0 mmol, 2.5 eq) and Pd(dppf)Cl ₂ (0.948 g, 1.30 mmol, 0.06 eq) in one portion at 25°C under N ₂ . The mixture was heated to 80°C and stirred for 16 h. The reaction mixture was filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 5-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan -2- yl)benzaldehyde (8 g, crude) as a white solid. ¹ H NMR (CDCl _3, 400 MHz) δ 10.73 (s, 1H), 8.40 (s, 1H), 8.24 (s, 1H), 8.11-8.08 (m, 1H), 8.07-8.03 (m, 1H), 7.86-7.80 (m, ₂ H), 7.49 (t, J = 6.8 Hz, 1H), 7.27 (t, J = 7.6 Hz, 1H), 1.43 (s, 12H). [0523] F14.6 Preparation of (1-hydroxy-6- indazol-1-yl-2,3,1-benzodiazaborinin-2- yl)- (5-methylthiazol-2-yl)methanone [0524] To a mixture of 5-indazol-1-yl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (300 mg, 861 umol, 1 eq) in EtOH (3 mL) was added 5-methylthiazole-2- carbohydrazide (135 mg, 861 umol, 1 eq) and NH ₃ .H ₂ O (1.95 mmol, 0.3 mL, 25% purity, 2.26 eq) in one portion at 20°C under N ₂ . The mixture was heated to 50°C and stirred for 2 h. The reaction mixture was concentrated under reduced pressure to give a residue. The residue was purified by prep-HPLC (column:Waters Xbridge Prep OBD C18150*40mm*10um ;mobile phase:water (0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN;B%: 20%-50%,7min) to give (1-hydroxy- 6- indazol-1-yl-2,3,1-benzodiazaborinin-2-yl)-(5-methylthiazol- 2-yl)methanone (73 mg, 188 umol, 21.9% yield) as a yellow solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.65 (s, 0.5H), 8.46 (s, 0.5H), 8.40 (s, 0.5H), 8.26 (s, 0.5H), 8.04 (s, 1H), 7.95-7.87 (m, 3H), 7.83-7.77 (m, 2H), 7.54- 7.50 (m, 1H), 7.32-7.27 (m, 1H), 2.57 (s, 3H). MS (ESI): mass calcd. For C19H14BN5O2S 387.10, m/z found 388.2 [M+H] ⁺ . HPLC: 97.18% (220 nm), 96.14% (254 nm). [0525] F15 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(2-methoxyphenyl)-2,3,1- benzodiazaborinin-2-yl]methanone [0527] To a mixture of (2-methoxyphenyl)boronic acid (5.00 g, 32.9 mmol, 1 eq) and 5- bromo-2-hydroxy-benzaldehyde (9.92 g, 49.3 mmol, 1.5 eq) in H ₂ O (150 mL) was added K ₂ CO ₃ (9.10 g, 65.8 mmol, 2 eq) and Pd(PPh3)4 (0.380 g, 329 umol, 0.01 eq) at 25°C under N ₂ . The resulting suspension was stirred at 80°C for 16 h. The mixture was filtered and the filtrate was extracted with ethyl acetate (100 mL x 3), the combined organic phase was washed with brine (50 mL), dried with anhydrous Na2SO4, filtered and concentrated in vacuum to give 2-hydroxy- 5-(2-methoxyphenyl)benzaldehyde (8 g, crude) as a brown solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.04 (br s, 1H), 9.94 (s, 1H), 7.75-7.72 (m, ₂ H), 7.38-7.30 (m, ₂ H), 7.08-7.00 (m, 3H), 3.85 (s, 3H). [0528] F15.2 Preparation of [2-formyl-4-(2-methoxyphenyl)phenyl] trifluoromethanesulfonate [0529] To a mixture of 2-hydroxy-5-(2-methoxyphenyl)benzaldehyde (2.00 g, 8.76 mmol, 1 eq) and pyridine (26.3 mmol, 2.1 mL, 3 eq) in DCM (20 mL) was added Tf ₂ O (13.1 mmol, 2.2 mL, 1.5 eq) drop-wise at 0°C, the mixture was stirred at 0°C for 2 h. The reaction mixture was quenched by addition sat.aq.NH ₄ Cl (40 mL) at 0°C, and extracted with DCM (30 mL x 2). The combined organic phase was washed with brine (30 mL), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=20/1 to 10/1) to give [2-formyl-4-(2-methoxyphenyl)phenyl] trifluoromethanesulfonate (1.7 g, 4.72 mmol, 53.8% yield) as a yellow oil. ¹ H NMR (CDCl _3, 400 MHz) δ 10.31 (s, 1H), 8.15 (d, J = 2.4 Hz, 1H), 7.89 (dd, J = 8.8, 2.4 Hz, 1H), 7.44 (d, J = 8.4 Hz, 1H), 7.41-7.38 (m, 1H), 7.34 (dd, J = 8.0, 2.0 Hz, 1H), 7.08 (t, J = 7.6 Hz, 1H), 7.03 (d, J = 8.4 Hz, 1H), 3.85 (s, 3H). [0530] F15.3 Preparation of 5-(2-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0531] To a mixture of [2-formyl-4-(2-methoxyphenyl)phenyl] trifluoromethanesulfonate (1.70 g, 4.72 mmol, 1 eq) and 4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane) (2.40 g, 9.44 mmol, 2 eq) in dioxane (50 mL) was added KOAc (1.16 g, 11.8 mmol, 2.5 eq) and Pd(dppf)Cl ₂ (0.173 g, 235 umol, 0.05 eq) in one portion at 25°C under N ₂ . The mixture was heated to 90°C and stirred for 16 h. The reaction mixture was filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 5-(2-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n- 2-yl)benzaldehyde (1.60 g, crude) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.63 (s, 1H), 8.14 (s, 1H), 7.92 (d, J = 7.6 Hz, 1H), 7.79 (dd, J = 7.6, 1.6 Hz, 1H), 7.38-7.33 (m, ₂ H), 7.05 (t, J = 7.2 Hz, 1H), 6.99 (d, J = 8.4 Hz, 1H), 3.80 (s, 3H), 1.41 (s, 12H). [0532] F15.4 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(2-methoxyphenyl)- 2,3,1- benzodiazaborinin-2-yl]methanone [0533] To a mixture of 5-(2-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n - 2-yl)benzaldehyde (400 mg, 1.18 mmol, 1 eq) in EtOH (3 mL) was added 2- chlorobenzohydrazide (201 mg, 1.18 mmol, 1 eq) and NH ₃ .H ₂ O (1.95 mmol, 0.3 mL, 25% purity, 1.65 eq) in one portion at 20°C under N ₂ . The mixture was heated to 50°C and stirred for 2 h. The reaction mixture was concentrated under reduced pressure to give a residue. The residue was purified by prep-HPLC (column: Phenomenex Gemini-NX C1875*30mm*3um;mobile phase: [water(0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 10%-40%,8min) to give (2- chlorophenyl)-[1-hydroxy-6-(2-methoxyphenyl)-2,3,1-benzodi azaborinin-2-yl]methanone (101 mg, 252 umol, 21.4% yield, 97.8% purity) as a white solid. ¹ H NMR (DMSO-d _6, 400 MHz) δ 8.17 (s, 1H), 7.81 (d, J = 7.6 Hz, 1H), 7.70-7.67 (m, 2H), 7.62-7.54 (m, 3H), 7.51-7.46 (m, 1H), 7.38 (t, J = 8.8 Hz, 1H), 7.33 (dd, J = 7.6, 1.6 Hz, 1H), 7.14 (d, J = 8.4 Hz, 1H), 7.06 (t, J = 7.2 Hz, 1H), 3.77 (s, 3H). MS (ESI): mass calcd. For C21H16BClN ₂ O3390.09, m/z found 391.2 [M+H] ⁺ . HPLC: 97.84% (220 nm), 98.63% (254 nm). [0534] F16 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(4-methoxyphenyl)-2,3,1- benzodiazaborinin-2-yl]methanone [0535] F16.1 Preparation of 2-hydroxy-5-(4-methoxyphenyl)benzaldehyde [0536] To a mixture of (4-methoxyphenyl)boronic acid (5.00 g, 32.9 mmol, 1 eq) and 5- bromo-2-hydroxy-benzaldehyde (9.92 g, 49.4 mmol, 1.5 eq) in H ₂ O (250 mL) was added K ₂ CO ₃ (9.10 g, 65.8 mmol, 2 eq) and Pd(PPh3)4 (380 mg, 329 umol, 0.01 eq) at 25°C under N ₂ . The resulting suspension was stirred at 80°C for 16 h. The reaction mixture was cooled to r.t., solid was precipitate out. The solid was collected and washed with H ₂ O (30 mL x 2) to give 2- hydroxy-5-(4-methoxyphenyl)benzaldehyde (9 g, crude) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.97 (s, 1H), 9.98 (s, 1H), 7.75-7.71 (m, ₂ H), 7.48 (d, J = 8.8 Hz, 2H), 7.06 (d, J = 8.4 Hz, 1H), 6.99 (d, J = 8.8 Hz, ₂ H), 3.87 (s, 3H). [0537] F16.2 Preparation of [2-formyl-4-(4-methoxyphenyl)phenyl] trifluoromethanesulfonate [0538] To a mixture of 2-hydroxy-5-(4-methoxyphenyl)benzaldehyde (3.00 g, 13.1 mmol, 1 eq) and pyridine (3.12 g, 39.4 mmol, 3.18 mL, 3 eq) in DCM (30 mL) was added Tf ₂ O (4.82 g, 17.1 mmol, 2.8 mL, 1.3 eq) drop-wise at 0°C. The mixture was stirred at 20°C for 2 h. The reaction mixture was poured into sat.aq.NH ₄ Cl (30 mL) and extracted with DCM (20 mL x 3). The combined organic phase was washed with brine (30 mL), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by flash silica gel chromatography (ISCO®; 40 g SepaFlash® Silica Flash Column, Eluent of 0~7% Ethyl acetate/Petroleum ethergradient @ 50 mL/min) to give [2-formyl-4-(4-methoxyphenyl)phenyl] trifluoromethanesulfonate (2.40 g, 6.66 mmol, 50.7% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.33 (s, 1H), 8.14 (d, J = 2.4 Hz, 1H), 7.86 (dd, J = 8.8, 2.4 Hz, 1H), 7.55 (d, J = 8.4 Hz, 2H), 7.45 (d, J = 8.4 Hz, 1H), 7.02 (d, J = 8.8 Hz, ₂ H), 3.88 (s, 3H). [0539] F16.3 Preparation of 5-(4-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0540] To a mixture of [2-formyl-4-(4-methoxyphenyl)phenyl] trifluoromethanesulfonate (2.40 g, 6.66 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2-yl) -1,3,2-dioxaborolane (2.54 g, 10.0 mmol, 1.5 eq) in dioxane (30 mL) was added Pd(dppf)Cl ₂ (244 mg, 333 umol, 0.05 eq) and KOAc (1.63 g, 16.7 mmol, 2.5 eq) at 25°C under N ₂ . The mixture was stirred at 80°C for 5 h. The reaction mixture was cooled to r.t. and filtered through a pad of celite. The filtrate was concentrated under reduced pressure to give a residue and the residue was purified by flash silica gel chromatography (ISCO®; 40 g SepaFlash® Silica Flash Column, Eluent of 5~10% Ethyl acetate/Petroleum ethergradient @ 40 mL/min) to give 5-(4- methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-y l)benzaldehyde (2 g, 5.91 mmol, 88.8% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.18 (s, 1H), 7.94 (d, J = 7.6 Hz, 1H), 7.78 (dd, J = 7.6, 1.6 Hz, 1H), 7.59 (d, J = 8.8 Hz, ₂ H), 6.99 (d, J = 8.8 Hz, 2H), 3.85 (s, 3H), 1.40 (s, 1 ₂ H). [0541] F16.4 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(4-methoxyphenyl)- 2,3,1- benzodiazaborinin-2-yl]methanone [0542] To a mixture of 5-(4-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2- yl) benzaldehyde (400 mg, 1.18 mmol, 1 eq) and 2-chlorobenzohydrazide (202 mg, 1.18 mmol, 1 eq) in EtOH (3 mL) was added NH ₃ .H ₂ O (0.3 mL) at 20°C. The mixture was stirred at 50°C for 1 h. The reaction mixture was cooled to 20°C and added H ₂ O (0.2 mL). The resulting solution was purified by prep-HPLC (column: Phenomenex Gemini-NX C1875*30mm*3um;mobile phase: [water(0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 10%-30%,8min) to give (2- chlorophenyl)-[1-hydroxy-6-(4-methoxyphenyl)-2,3,1- benzodiazaborinin-2-yl]methanone (198 mg, 504 umol, 42.6% yield, 99.38% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.19 (s, 1H), 7.88 (s, 1H), 7.84 (s, ₂ H), 7.67 (d, J = 8.8, 2.4 Hz, ₂ H), 7.60-7.58 (m, 1H), 7.57- 7.56 (m, 1H), 7.56-7.54 (m, 1H), 7.05 (d, J = 8.4, 1.6 Hz, ₂ H), 3.81 (s, 3H). MS (ESI): mass calcd. For C21H16BClN ₂ O3390.09, m/z found 391.2 [M+H] ⁺ . HPLC: 99.38% (220 nm), 99.51% (254 nm). [0543] F17 Preparation of (2-chlorophenyl)-[6-(3-chlorophenyl)-1-hydroxy-2,3,1- benzodiazaborinin-2-yl]methanone

[0545] To a mixture of (3-chlorophenyl)boronic acid (5.00 g, 31.9 mmol, 1 eq) and 5- bromo-2-hydroxy-benzaldehyde (9.64 g, 47.9 mmol, 1.5 eq) in H ₂ O (150 mL) was added K ₂ CO ₃ (8.84 g, 63.9 mmol, 2 eq) and Pd(PPh ₃ ) ₄ (0.369 g, 319 umol, 0.01 eq) at 25°C. The resulting suspension was stirred at 80°C for 16 h. The mixture was filtered and the filtrate was extracted with ethyl acetate (100 mL x 3), the combined organic phase was washed with brine (50 mL), dried with anhydrous Na2SO4, filtered and concentrated in vacuum to give 5-(3-chlorophenyl)- 2-hydroxy-benzaldehyde (9.00 g, crude) as a brown solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 10.91 (br s, 1H), 10.31 (s, 1H), 7.94 (d, J = 2.4 Hz, 1H), 7.86 (dd, J = 8.4, 2.4Hz, 1H), 7.67 ( s, 1H), 7.58 (d, J = 7.6 Hz, 1H), 7.45 (t, J = 8.0 Hz, 1H), 7.37 (d, J = 7.6 Hz, 1H), 7.09 (d, J = 8.4 Hz, 1H). [0546] F17.2 Preparation of [4-(3-chlorophenyl)-2-formyl-phenyl] trifluoromethanesulfonate [0547] To a mixture of 5-(3-chlorophenyl)-2-hydroxy-benzaldehyde (8.00 g, 34.4 mmol, 1 eq) and pyridine (103 mmol, 8.3 mL, 3 eq) in DCM (100 mL) was added Tf ₂ O ( 44.7 mmol, 7.4 mL, 1.3 eq) drop-wise at 0°C, the mixture was stirred at 0°C for 1 h. The reaction mixture was quenched by addition sat.aq.NH ₄ Cl (150 mL) at 0°C and extracted with DCM (100 mL x 2). The combined organic phase was washed with brine (100 mL ), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by column chromatography (SiO2, Petroleum ether/Ethyl acetate=20/1 to 10/1) to give [4-(3-chlorophenyl)-2-formyl - phenyl] trifluoromethanesulfonate (9.00 g, 24.7 mmol, 71.8% yield) as yellow oil. ¹ H NMR (DMSO-d6, 400 MHz) δ 10.15 ( s, 1H), 8.47 (s, 1H), 8.19 (dd, J = 8.8, 2.8 Hz, 1H), 7.88 (s, 1H), 7.78-7.74 (m, 1H), 7.68 (d, J = 8.4 Hz, 1H), 7.56-7.52 (m, ₂ H). [0548] F17.3 Preparation of 5-(3-chlorophenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0549] To a mixture of [4-(3-chlorophenyl)-2-formyl-phenyl] trifluoromethanesulfonate (8.00 g, 21.9 mmol, 1 eq) and 4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane) (8.35 g, 32.9 mmol, 1.5 eq) in dioxane (150 mL) was added KOAc (5.38 g, 54.8 mmol, 2.5 eq) and Pd(dppf)Cl ₂ (0.481 g, 658 umol, 0.03 eq) in one portion at 25°C under N ₂ . The mixture was heated to 80°C and stirred for 16 h. The reaction mixture was filtered and the filtrate was concentrated in vacuum. The residue was purified by column chromatography (SiO ₂ , Petroleum ether/Ethyl acetate=10/1 to 5/1) to give 5-(3-chlorophenyl)-2-(4,4,5,5-tetramethyl-1,3,2 - dioxaborolan-2-yl)benzaldehyde (7.00 g, 20.4 mmol, 93.1% yield) as a white solid. ¹ H NMR (CDCl _3, 400 MHz) δ 10.67 (s, 1H), 8.19 (s, 1H), 7.98 (d, J = 8.0 Hz, 1H), 7.80 (dd, J = 7.6, 2.0 Hz, 1H), 7.64 (s, 1H), 7.55-7.51 (m, 1H), 7.41-7.37 (m, ₂ H), 1.42 (s, 12H). [0550] F17.4 Preparation of (2-chlorophenyl)-[6-(3-chlorophenyl)-1-hydroxy-2,3,1- benzodiazaborinin-2-yl]methanone [0551] To a mixture of 5-(3-chlorophenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan -2-yl) benzaldehyde (400 mg, 1.17 mmol, 1 eq) in EtOH (3 mL) was added 2-chlorobenzohydrazide (199 mg, 1.17 mmol, 1 eq) and NH ₃ .H ₂ O (1.92 mmol, 0.3 mL, 25% purity, 1.65 eq) in one portion at 20°C under N ₂ . The mixture was heated to 50°C and stirred for 2 h. The reaction mixture was concentrated under reduced pressure to give a residue. The residue was purified by prep-HPLC (column: Phenomenex Gemini-NX C1875*30mm*3um;mobile phase: [water(0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 15%-35%,8min) to give (2-chlorophenyl)- [6-(3-chlorophenyl)-1-hydroxy-2,3,1-benzodiazaborinin-2-yl]m ethanone (185 mg, 461 umol, 39.5% yield, 98.4% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.21 (s, 1H), 8.00 (s, 1H), 7.94-7.91 (m, 1H), 7.90-7.87 (m, 1H), 7.80 (s, 1H), 7.71 (d, J = 7.6 Hz, 1H), 7.62-7.53 (m, 4H), 7.52-7.45 (m, 3H). MS (ESI): mass calcd. For C20H13BCl ₂ N ₂ O2394.04, m/z found 395.1 [M+H] ⁺ . HPLC: 98.44% (220 nm), 99.18% (254 nm). [0552] F18 Preparation of (2-chlorophenyl)-[1-hydroxy-7-[5-(trifluoromethyl)-1,2,4- oxadiazol -3-yl]-2,3,1-benzodiazaborinin-2-yl]methanone [0553] F18.1 Preparation of 2-(2-bromo-4-fluoro-phenyl)-1,3-dioxolane [0554] To a solution of 2-bromo-4-fluoro-benzaldehyde (25.0 g, 123 mmol, 1 eq) in toluene (300 mL) was added TsOH.H ₂ O (11.7 g, 61.6 mmol, 0.5 eq) and ethylene glycol (8.41 g, 135 mmol, 7.60 mL, 1.1 eq). The mixture was stirred at 130°C for 12 h. The reaction mixture was added H ₂ O (100 mL) and extracted with EtOAc (2 x 100 mL). The combined organic layers were washed with brine (50 mL x 3), dried over Na2SO4, filtered and concentrated under reduced pressure. The residue was purified by flash silica gel chromatography (ISCO®; 220 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 2-(2-bromo-4-fluoro-phenyl)-1,3-dioxolane (12.0 g, 39.4% yield) as brown oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 7.60 (dd, J = 8.8, 6.4 Hz, 1H ), 7.32 (dd, J = 8.0, 2.4 Hz, 1H ), 7.08 (td, J = 8.0, 2.4 Hz, 1H ), 6.05 (s, 1H), 4.16-4.14 (m, 2H), 4.09-4.07 (m, ₂ H). [0555] F18.2 Preparation of 3-bromo-4-(1,3-dioxolan-2-yl)benzonitrile [0556] To a solution of 2-(2-bromo-4-fluoro-phenyl)-1,3-dioxolane (6.00 g, 24.3 mmol, 1 eq) in DMSO (60 mL) was added cyanopotassium (2.40 g, 36.4 mmol, 1.5 eq) in portions at 20°C. The mixture was stirred at 140°C for 12 h. The reaction mixture was quenched by H ₂ O (50 mL). The mixture was adjusted to pH=8 by sat.NaHCO3 and extracted with EtOAc (50 mL x 3). The combined organic phase was washed with brine (50 mL x 3), dried with anhydrous Na2SO4, filtered and concentrated in vacuum. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 3-bromo-4-(1,3-dioxolan-2-yl) benzonitrile (3.40 g, 27.5% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 7.87 (d, J = 1.2 Hz, 1H), 7.72 (d, J = 8.0 Hz, 1H), 7.64 (dd, J = 8.0, 1.2 Hz, 1H), 6.08 (s, 1H), 4.17-4.14 (m, 2H), 4.12-4.10 (m, 2H). [0557] F18.3 Preparation of 3-bromo-4-(1,3-dioxolan-2-yl)-N'-hydroxy-benzamidine [0558] To a solution of 3-bromo-4-(1,3-dioxolan-2-yl)benzonitrile (3.30 g, 13.0 mmol, 1 eq) in H ₂ O (24 mL) and EtOH (12 mL) was added NH ₂ OH.HCl (2.30 g, 32.5 mmol, 2.5 eq) and K ₂ CO ₃ (2.70 g, 19.5 mmol, 1.5 eq) in one portion at 20°C. The mixture was stirred at 90°C for 6 h. The reaction mixture was quenched with sat.NH ₄ Cl (30 mL) and extracted with EtOAc (30 mL x 3). The combined organic layers were washed with brine (30 mL x 3), dried over Na ₂ SO ₄ , filtered and concentrated under reduced pressure to give 3-bromo-4-(1,3-dioxolan- 2-yl)-N'- hydroxy-benzamidine (3.20 g, 85.8% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 7.86 (d, J = 1.2 Hz, 1H), 7.65-7.59 (m, ₂ H), 6.10 (s, 1H), 4.86 (s, 2H), 4.17-4.15 (m, 2H), 4.11-4.09 (m, 2H). [0559] F18.4 Preparation of 3-[3-bromo-4-(1,3-dioxolan-2-yl)phenyl]-5- (trifluoromethyl)-1,2,4- oxadiazole [0560] To a solution of 3-bromo-4-(1,3-dioxolan-2-yl)-N'-hydroxy-benzamidine (3.20 g, 11.0 mmol, 1 eq) in DMF (50 mL) was added pyridine (2.60 g, 33.1 mmol, 2.70 mL, 3 eq) and TFAA (2.80 g, 13.3 mmol, 1.80 mL, 1.2 eq) dropwise at 0°C. After addition, the mixture was stirred at 0°C for 15 min. And then the resulting mixture was stirred at 85°C for 4 h. The reaction mixture was quenched with water (50 mL) at 0°C, and adjusted to pH=5 with HCl (2N). The resulting mixture was extracted with EtOAc (50 mL x 3). The combined organic layers were washed with brine (50 mL x 3), dried over Na ₂ SO ₄ , filtered and concentrated under reduced pressure. The residue was purified by flash silica gel chromatography (ISCO®; 20 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 50 mL/min) to give 3-[3-bromo-4-(1,3-dioxolan-2-yl)phenyl]-5-(trifluoromethyl)- 1,2,4- oxadiazole (2.50 g, 62.0% yield) as a white solid. ¹ H NMR (MeOD, 400 MHz) δ 8.29 (d, J = 1.6 Hz, 1H), 8.10 (dd, J = 8.0, 1.6 Hz, ₂ H), 7.78 (d, J = 8.0, 1H), 6.07 (s, 1H), 4.19-4.14 (m, 2H), 4.08-4.06 (m, 2H). [0561] F18.5 Preparation of 2-bromo-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3- yl]benzaldehyde [0562] To a solution of 3-[3-bromo-4-(1,3-dioxolan-2-yl)phenyl]-5-(trifluoromethyl)- 1,2,4- oxadiazole (2.50 g, 6.90 mmol, 1 eq) in THF (15 mL) was added HCl (2 N, 13.7 mL, 4 eq) dropwise at 20°C. The mixture was stirred at 40°C for 4 h. The mixture was adjusted to pH=7 by sat. NaHCO ₃ and then concentrated to remove the THF. The residue was diluted with H ₂ O (20 mL) and extracted with EtOAc (20 mL x 3). The combined organic layers were washed with brine (30 mL), dried over Na ₂ SO ₄ , filtered and concentrated under reduced pressure. The residue was purified by flash silica gel chromatography (ISCO®; 25 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 2- bromo-4-[5-(trifluoromethyl)-1,2,4 -oxadiazol-3-yl]benzaldehyde (1.80 g, 81.9% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.42 (s, 1H), 8.45 (d, J = 1.2 Hz, 1H), 8.20 (dd, J = 8.0, 1.2 Hz, 1H), 8.06 (d, J = 8.0 Hz, 1H). [0563] F18.6 Preparation of 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-4-[5- (trifluoromethyl)-1,2,4- oxadiazol-3-yl]benzaldehyde [0564] A mixture of 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-5,5-dimethyl-1,3,2- dioxaborinane (422 mg, 1.87 mmol, 3 eq), 2-bromo-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3- yl]benzaldehyde (200 mg, 623 umol, 1 eq), Pd(dppf)Cl ₂ (91 mg, 124.59 umol, 0.2 eq), KOAc (183 mg, 1.87 mmol, 3 eq) in dioxane (5 mL) was degassed and purged with N ₂ for 3 times, and then the mixture was stirred at 80°C for 1 h under N ₂ atmosphere. The reaction mixture was filtered and concentrated under reduced pressure to give a residue containing 2-(5,5-dimethyl- 1,3,2-dioxaborinan-2-yl)-4-[5-(trifluoromethyl)-1,2,4- oxadiazol-3-yl]benzaldehyde. [0565] F18.7 Preparation of (2-chlorophenyl)-[1-hydroxy-7-[5-(trifluoromethyl)- 1,2,4-oxadiazol -3-yl]-2,3,1-benzodiazaborinin-2-yl]methanone [0566] To a mixture of 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-4-[5-(trifluorometh yl)- 1,2,4- oxadiazol -3-yl]benzaldehyde (200 mg, 237 umol, 1 eq) and 2-chlorobenzohydrazide (40 mg, 237 umol, 1 eq) in EtOH (2 mL) was dropwise added NH ₃ .H ₂ O (133 mg, 949 umol, 0.16 mL, 25% purity, 4 eq), then the mixture was stirred at 60°C for 3 h under N ₂ atmosphere. The reaction mixture was concentrated under reduced pressure. The residue was purified by prep- HPLC (column: Phenomenex Gemini-NX C1875*30mm*3um;mobile phase: [water(0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 10%-40%,8min) to give (2-chlorophenyl)- [1-hydroxy-7-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]-2,3, 1-benzodiazaborinin-2- yl]methanone (62 mg, 31.07% yield, 92.12% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.45 (d, J = 1.6 Hz, 1H), 8.33 (s, 1H), 8.24 (dd, J = 8.0, 1.6 Hz, 1H), 7.88 (d, J = 8.0 Hz, 1H), 7.62-7.60 (m, 3H), 7.58-7.41 (m, ₂ H). MS (ESI): mass calcd. For C17H9BClF3N4O3420.04, m/z found 421.1 [M+H] ⁺ . HPLC: 92.12% (220 nm), 92.66% (254 nm). [0567] F19 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(3-methylsulfanylphenyl)- 2,3,1- benzodiazaborinin-2-yl] methanone [0568] F19.1 Preparation of 2-hydroxy-5-(3-methylsulfanylphenyl)benzaldehyde [0569] To a mixture of (3-methylsulfanylphenyl)boronic acid (10.0 g, 60 mmol, 1 eq) and 5-bromo-2-hydroxy-benzaldehyde (18.0 g, 89 mmol, 1.5 eq) in H ₂ O (300 mL) was added K ₂ CO ₃ (16.5 g, 119 mmol, 2 eq) and Pd(PPh3)4 (0.688 g, 595 umol, 0.01 eq) at 25°C under N ₂ . The resulting suspension was stirred at 80°C for 16 h. The reaction mixture was poured into ice- water (50 mL). The aqueous phase was extracted with ethyl acetate (100 mL x 3). The combined organic phase was washed with brine (100 mL), dried with anhydrous Na2SO4, filtered and concentrated in vacuum. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 2-hydroxy-5-(3- methylsulfanylphenyl) benzaldehyde (2.2 g, 9 mmol, 15.1% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.03 (s, 1H), 9.99 (s, 1H), 7.78-7.75 (m, 2H), 7.44 (s, 1H), 7.39-7.32 (t, J = 7.6 Hz, 1H), 7.32 (d, J = 8.0 Hz, 1H), 7.25 (d, J = 8.0 Hz, 1H), 7.09 (d, J = 9.2 Hz, 1H), 2.55 (s, 3H). [0570] F19.2 Preparation of [2-formyl-4-(3-methylsulfanylphenyl)phenyl] trifluoromethanesulfonate [0571] To a mixture of 2-hydroxy-5-(3-methylsulfanylphenyl)benzaldehyde (2.20 g, 9 mmol, 1 eq) and pyridine (2.14 g, 27 mmol, 2.2 mL, 3 eq) in DCM (20 mL) was added Tf ₂ O (3.30 g, 11.7 mmol, 1.9 mL, 1.3 eq) drop-wise at 0°C over 10 min. The mixture was stirred at 20°C for 2 h. The reaction mixture was poured into sat.aq.NH4Cl (30 mL). The aqueous phase was extracted with DCM (20 mL x 3). The combined organic phase was washed with brine (40 mL), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by flash silica gel chromatography (ISCO®; 40 g SepaFlash® Silica Flash Column, Eluent of 0~7% Ethyl acetate/Petroleum ethergradient @ 40 mL/min) to give [2-formyl-4-(3- methylsulfanylphenyl)phenyl]trifluoromethanesulfonate (2.9 g, 7.7 mmol, 85.6% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.30 (s, 1H), 8.12 (d, J = 2.4 Hz, 1H), 7.85 (dd, J = 8.8, 2.8 Hz, 1H), 7.46 (d, J = 8.4 Hz, 1H), 7.42-7.39 (m, 1H), 7.36 (d, J = 7.6 Hz, 1H), 7.32-7.28 (m, ₂ H), 2.51 (s, 3H). [0572] F19.3 Preparation of 5-(3-methylsulfanylphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan -2-yl)benzaldehyde [0573] To a mixture of [2–formyl-4-(3-methylsulfanylphenyl)phenyl] trifluoromethanesulfonate (2.9 g, 7.70 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl) -1,3,2-dioxaborolane (2.93 g, 11.6 mmol, 1.5 eq) in dioxane (30 mL) was added Pd(dppf)Cl ₂ (0.282 g, 385 umol, 0.05 eq) and KOAc (1.89 g, 19.3 mmol, 2.5 eq) at 25°C under N ₂ . The mixture was stirred at 80°C for 5 h. The reaction mixture was cooled to r.t. and filtered with celite, the filtrate was concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 40 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 40 mL/min) to give 5-(3-methylsulfanylphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-diox aborolan -2- yl)benzaldehyde (2 g, 5.70 mmol, 73.3% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.64 (s, 1H), 8.17 (s, 1H), 7.94 (d, J = 7.6 Hz, 1H), 7.78 (dd, J = 7.6, 2.0 Hz, 1H), 7.49 (s, 1H), 7.40-7.34 (m, 2H), 7.27-7.24 (m, H), 2.52 (s, 3H), 1.38 (s, 1 ₂ H). [0574] F19.4 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(3- methylsulfanylphenyl)-2,3,1- benzodiazaborinin-2-yl] methanone [0575] To a mixture of 5-(3-methylsulfanylphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde (500 mg, 1.4 mmol, 1 eq) and 2-chlorobenzohydrazide (241 mg, 1.4 mmol, 1 eq) in EtOH (3.5 mL) was added NH ₃ .H ₂ O (0.3 mL) at 20°C. The mixture was stirred at 50°C for 1 h. The reaction mixture was cooled to 20°C and added H ₂ O (0.2 mL). The resulting mixture was purified by prep-HPLC (column: Phenomenex Gemini-NX C18 75*30mm*3um;mobile phase: [water(0.05%NH3H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 15%- 38%,8min) to give (2-chlorophenyl)-[1-hydroxy-6-(3-methylsulfanylphenyl)-2,3,1 - benzodiazaborinin-2-yl] methanone (307 mg, 746 umol, 52.9% yield, 98.89% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.22 (s, 1H), 7.96 (s, 1H), 7.90-7.88 (m, ₂ H), 7.60- 7.54 (m, 4H), 7.51-7.42 (m, 4H), 7.31-7.29 (m, 1H), 2.54 (s, 3H). MS (ESI): mass calcd. For C21H16BClN ₂ O2S 406.07, m/z found 407.2 [M+H] ⁺ . HPLC: 98.89% (220 nm), 97.91% (254 nm). [0576] F20 Preparation of (2-chlorophenyl)-(1-hydroxy-7-phenyl-2,3,1- benzodiazaborinin-2-yl) methanone [0577] F20.1 Preparation of 2-hydroxy-4-phenyl-benzaldehyde [0578] To a mixture of 4-bromo-2-hydroxy-benzaldehyde (5.00 g, 24.9 mmol, 1 eq) and phenylboronic acid (3.64 g, 29.9 mmol, 1.2 eq) in H ₂ O (100 mL) was added K ₂ CO ₃ (6.88 g, 49.8 mmol, 2 eq) and Pd(PPh3)4 (0.072 g, 62.2 umol, 0.0025 eq) at 25°C under N ₂ . The mixture was stirred at 80°C for 12 h. The mixture was adjusted pH to 7 with 2N HCl and extracted with EtOAc (50 mL x 3). The combined organic layers were washed with brine (20 mL x 3), dried over Na2SO4, filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 2-hydroxy-4- phenyl-benzaldehyde (4.4 g, 22.2 mmol, 89.24% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.16 (s, 1H), 9.97 (s, 1H), 7.68-7.65 (m, 3H), 7.54-7.45 (m, 4H), 7.31-7.30 (m, 1H). [0579] F20.2 Preparation of (2-formyl-5-phenyl-phenyl) trifluoromethanesulfonate [0580] To a mixture of 2-hydroxy-4-phenyl-benzaldehyde (4.40 g, 22.2 mmol, 1 eq) and Pyridine (66.6 mmol, 5.4 mL, 3 eq) in DCM (80 mL) was added Tf ₂ O ( 33.3 mmol, 5.5 mL, 1.5 eq) drop-wise at 0°C, the mixture was stirred at 0°C for 2 h. The reaction mixture was poured into sat aq. NH4Cl (100 mL), and extracted with DCM (50 mL x 3). The combined organic layers were washed with brine (20 mL x 3), dried over Na2SO4, filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give (2-formyl-5-phenyl-phenyl) trifluoromethanesulfonate (7 g, 21.2 mmol, 95.48% yield) a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.31 (s, 1H), 8.08 (d, J = 8.4 Hz, 1H), 7.78 (dd, J = 8.0, 1.2 Hz, 1H), 7.64-7.63(m, 1H), 7.62-7.61 (m, ₂ H), 7.55- 7.49 (m, 3H). [0581] F20.3 Preparation of 4-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde [0582] To a solution of (2-formyl-5-phenyl-phenyl) trifluoromethanesulfonate (3.00 g, 9.08 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2-yl)-1,3,2 - dioxaboro lane (4.61 g, 18.2 mmol, 2 eq) in dioxane (60 mL) was added Pd(dppf)Cl ₂ (0.332 g, 454umol, 0.05 eq) and KOAc (1.78 g, 18.2 mmol, 2 eq) at 25°C under N ₂ , the mixture was stirred at 80°C for 6 h. The reaction mixture was filtered and the filtrate was concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 40 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 80 mL/min) to give 4-phenyl-2-(4,4,5,5-tetramethyl -1,3,2-dioxaborolan-2- yl)benzaldehyde (2.60 g, 8.44 mmol, 92.88% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.59 (s, 1H), 8.08 (d, J = 2.0 Hz, 1H), 8.05 (d, J = 8.0 Hz, 1H), 7.79 (dd, J = 8.4, 2.0 Hz, 1H), 7.68 (s, 1H), 7.66 (s, 1H), 7.48 (t, J = 7.6 Hz, ₂ H), 7.41 (t, J = 8.8 Hz, 1H), 1.42 (s, 1 ₂ H). [0583] F20.4 Preparation of (2-chlorophenyl)-(1-hydroxy-7-phenyl-2,3,1- benzodiazaborinin-2-yl) methanone [0584] To a solution of 4-phenyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (500 mg, 1.62 mmol, 1 eq) in EtOH (4 mL) was added 2-chlorobenzohydrazide (277 mg, 1.62 mmol, 1 eq) and NH ₃ .H ₂ O (3.24 mmol, 500 uL, 25% purity, 2 eq) at 25°C, the mixture was stirred at 50°C for 2 h. The precipitate was formed, the precipitate was filtered under reduced pressure to give a residue. The crude product was triturated with EtOH (5 mL) at 25 ^o C to give (2-chlorophenyl)-(1-hydroxy-7-phenyl-2,3,1-benzodiazaborinin -2- yl)methanone (273 mg, 713 umol, 43.92% yield, 94.12% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.04 (s, 1H), 7.74 (d, J =7.2 Hz, ₂ H), 7.61 (dd, J =8.0, 2.0 Hz, 1H), 7.49 (t, J =8.0 Hz, 2H), 7.44-7.39 (m, ₂ H), 7.38-7.32 (m, 4H), 7.32-7.26 (m, 2H). MS (ESI): mass calcd. For C20H14BClN ₂ O2360.08, m/z found 361.2 [M+H] ⁺ . HPLC: 94.12% (220 nm), 94.64% (254 nm). [0585] F21 Preparation of [1-hydroxy-7-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]- 2,3,1- benzodiazaborinin-2-yl]-(5-methylthiazol-2-yl)methanone [0586] To a mixture of 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-4-[5-(trifluorometh yl)- 1,2,4- oxadiazol-3-yl]benzaldehyde (400 mg, 474 umol, 42% purity, 1 eq) and 5-methylthiazole - 2-carbohydrazide (75 mg, 474 umol, 1 eq) in EtOH (2 mL) was added NH ₃ .H ₂ O (266 mg, 1.90 mmol, 292 uL, 25% purity, 4 eq) dropwise, the mixture was stirred at 60°C for 3 h under N ₂ atmosphere. The reaction mixture was concentrated under reduced pressure to remove EtOH. The residue was purified by prep-HPLC (column: Waters Xbridge Prep OBD C18 150*40mm*10um;mobile phase: [water(0.05%NH ₃ H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 15%- 45%,8min) to give [1-hydroxy-7-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]-2,3, 1- benzodiazaborinin-2-yl]-(5-methylthiazol-2-yl)methanone (40 mg, 9.08% yield, 87.66% purity) as a white solid. ¹ H NMR (DMSO-d ₆ , 400 MHz) δ 8.62 (s, 1H), 8.38 (s, 1H), 8.30 (d, J = 8.0 Hz, 1H), 8.01 (d, J = 8.0 Hz, 1H), 7.87 (s, 1H), 5.57 (s, 3H). MS (ESI): mass calcd. For C ₁₅ H ₉ BF ₃ N ₅ O ₃ S 407.05, m/z found 408.1 [M+H] ⁺ . HPLC: 87.66% (220 nm), 87.49% (254 nm). [0587] F22 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(3-methoxyphenyl)-2,3,1- benzodiazaborinin-2-yl]methanone

[0589] To a mixture of (3-methoxyphenyl)boronic acid (10.0 g, 65.8 mmol, 1 eq) and 5- bromo-2-hydroxy-benzaldehyde (13.9 g, 69.1 mmol, 1.05 eq) in H ₂ O (300 mL) was added K ₂ CO ₃ (18.2 g, 132 mmol, 2 eq) and Pd(PPh ₃ ) ₄ (0.190 g, 165 umol, 0.0025 eq) at 25°C under N ₂ . The mixture was stirred at 80°C for 12 h. The mixture was extracted with EtOAc (150 mL x 3). The combined organic layers were washed with brine (50 mL x 3), dried over Na2SO4, filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 220 g SepaFlash® Silica Flash Column, Eluent of 0~15% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 2-hydroxy-5-(3- methoxyphenyl)benzaldehyde (14.5 g, 63.5 mmol, 96.54% yield) as yellow gum. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.02 (s, 1H), 9.98 (s, 1H), 7.79-7.76 (m, 2H), 7.38 (t, J = 8.0 Hz, 1H), 7.15 (d, J = 8.0 Hz, 1H), 7.09-7.07 (m, 2H), 6.92 (dd, J = 8.4, 2.4 Hz, 1H), 3.88 (s, 3H). [0590] F22.2 Preparation of [2-formyl-4-(3-methoxyphenyl)phenyl] trifluoromethanesulfonate [0591] To a mixture of 2-hydroxy-5-(3-methoxyphenyl)benzaldehyde (5.00 g, 21.9 mmol, 1 eq) and pyridine (65.7 mmol, 5.3 mL, 3 eq) in DCM (60 mL) was added Tf ₂ O (32.9 mmol, 5.4 mL, 1.5 eq) drop-wise at 0°C, the mixture was stirred at 0°C for 2 h. The reaction mixture was poured into sat.aq.NH ₄ Cl 100 (mL) and extracted with DCM (40 mL x 3). The combined organic layers were washed with brine (20 mL x 3), dried over Na ₂ SO ₄ , filtered and concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; ISCO®; 80 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give [2-formyl-4-(3- methoxyphenyl)phenyl] trifluoromethanesulfonate (7 g, 19.4 mmol, 88.69% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.34 (s, 1H), 8.19 (d, J = 2.4 Hz, 1H), 7.90 (dd, J = 8.8, 2.8 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 7.42 (t, J = 8.0 Hz, 1H), 7.18 (d, J = 7.2 Hz, 1H), 7.12 (s, 1H), 6.99 (dd, J = 8.4, 2.8 Hz, 1H), 3.89 (s, 3H). [0592] F22.3 Preparation of 5-(3-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl) benzaldehyde [0593] To a solution of [2-formyl-4-(3-methoxyphenyl)phenyl] trifluoromethanesulfonate (7.00 g, 19.4 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2-yl) -1,3,2-dioxaborolane (9.87 g, 38.9 mmol, 2 eq) in dioxane (150 mL) was added Pd(dppf)Cl ₂ (0.711 g, 971. umol, 0.05 eq) and KOAc (3.81 g, 38.8 mmol, 2 eq) at 25°C under N ₂ , the mixture was stirred at 80°C for 6 h. The reaction mixture was filtered and the filtrate was concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 120 g SepaFlash® Silica Flash Column, Eluent of 0~15% Ethyl acetate/Petroleum ethergradient @ 100 mL/min) to give 5-(3-methoxyphenyl)-2-(4,4,5,5- tetramethyl-1,3,2- dioxaborolan-2-yl)benzaldehyde (5 g, 14.8 mmol, 76.10% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.22 (s, 1H), 7.97 (d, J = 8.0 Hz, 1H), 7.83 (dd, J = 8.0 , 2.0 Hz, 1H), 7.39 (t, J = 8.0 Hz, 1H), 7.25 (d, J = 8.0 Hz, 1H), 7.18 (s, 1H), 6.95 (dd, J = 8.4, 2.4 Hz, 1H), 3.89 (s, 3H), 1.42 (s, 1 ₂ H). [0594] F22.4 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(3-methoxyphenyl)- 2,3,1-benzodiazaborinin-2-yl]methanone [0595] To a solution of 5-(3-methoxyphenyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n- 2-yl) benzaldehyde (300 mg, 887 umol, 1 eq) in EtOH (3 mL) was added NH ₃ .H ₂ O (2.66 mmol, 0.4 mL uL, 25% purity, 3 eq) and 2-chlorobenzohydrazide (151 mg, 887 umol, 1 eq) at 25°C, the mixture was stirred at 50°C for 2 h. H ₂ O (0.1 mL) was added to the reaction mixture and the reaction mixture was purified by prep-HPLC (column: Kromasil C18 (250*50mm*10 um);mobile phase: [water(10mM NH ₄ HCO ₃ )-ACN];B%: 20%-50%,10min) to give (2-chlorophenyl)-[1- hydroxy-6-(3-methoxyphenyl) -2,3,1-benzodiazaborinin-2-yl]methanone (150 mg, 362.61 umol, 40.88% yield, 94.43% purity) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 8.21 (s, 1H), 7.95 (s, 1H), 7.91-7.85 (m, ₂ H), 7.62-7.53 (m, 4H), 7.51-7.47 (m, 1H), 7.42 (t, J = 8.4 Hz, 1H), 7.29 (t, J = 7.6 Hz, 1H), 7.26-7.24 (m, 1H), 7.42 (dd, J = 8.4, 2.0 Hz, 1H), 3.84 (s, 3H). MS (ESI): mass calcd. For C21H16BClN ₂ O3390.09, m/z found 391.1 [M+H] ⁺ . HPLC: 94.43% (220 nm), 98.88% (254 nm). [0596] F23 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(3-pyridyl)-2,3,1- benzodiazaborinin- 2-yl]methanone [0597] F23.1 Preparation of 2-hydroxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl) benzaldehyde [0598] To a mixture of 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2- yl) -1,3,2-dioxaborolane (30.3 g, 119 mmol, 1.2 eq) and 5-bromo-2-hydroxy-benzaldehyde (20.0 g, 99.5 mmol, 1 eq) in dioxane (200 mL) was added Pd(dppf)Cl ₂ (1.46 g, 1.99 mmol, 0.02 eq) and KOAc (29.3 g, 298 mmol, 3 eq) at 25°C under N ₂ . The mixture was stirred at 85°C for 16 h. The reaction mixture was cooled to r.t. and filtered through a pad of celite. The filtrate was concentrated under reduced pressure to give a residue and the residue was purified by flash silica gel chromatography (ISCO®; 220 g SepaFlash® Silica Flash Column, Eluent of 0~10% Ethyl acetate/Petroleum ethergradient @ 200 mL/min) to give 2-hydroxy-5-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)benzaldehyde (23.0 g, 92.7 mmol, 93.2% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.22 (s, 1H), 9.92 (s, 1H), 8.04 (s, 1H), 7.94 (d, J = 8.4 Hz, 1H), 6.97 (d, J = 8.4 Hz, 1H), 1.35 (s, 1 ₂ H). [0599] F23.2 Preparation of 2-hydroxy-5-(3-pyridyl)benzaldehyde [0600] To a mixture of 2-hydroxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (10.0 g, 40.3 mmol, 1 eq) and 3-bromopyridine (6.37 g, 40.3 mmol, 3.9 mL, 1 eq) in dioxane (100 mL) and H ₂ O (10 mL) was added K ₂ CO ₃ (13.9 g, 101 mmol, 2.5 eq) and Pd(PPh3)4 (0.466 g, 403 umol, 0.01 eq) at 25°C under N ₂ . The resulting suspension was stirred at 90°C for 4 h. The reaction mixture was poured into ice-water (w/w = 1/1) (10 mL). The aqueous phase was extracted with ethyl acetate (100 mL x 3). The combined organic phase was washed with brine (100 mL), dried with anhydrous Na2SO4, filtered and concentrated in vacuum. The crude product was triturated with MTBE (70 mL) at 20 ^o C for 30 min to give 2- hydroxy-5-(3-pyridyl)benzaldehyde (4.00 g, 20.1 mmol, 49.8% yield) as a yellow solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 11.08 (s, 1H), 10.01 (s, 1H), 8.84 (s, 1H), 8.62 (d, J = 4.8 Hz, 1H), 7.87-7.85 (m, 1H), 7.78-7.75 (m, ₂ H), 7.39 (dd, J = 7.6 Hz, 4.81H), 7.13 (d, J = 8.4 Hz, 1H). [0601] F23.3 Preparation of [2-formyl-4-(3-pyridyl)phenyl] trifluoromethanesulfonate [0602] To a mixture of 2-hydroxy-5-(3-pyridyl)benzaldehyde (4.00 g, 20.1 mmol, 1 eq) in CH3CN (100 mL) was added K ₂ CO ₃ (16.7 g, 120 mmol, 6 eq) and 1,1,1-trifluoro-N-phenyl-N- (trifluoromethylsulfonyl)methanesulfonamide (11.5 g, 32.1 mmol, 1.6 eq) drop-wise at 0°C. The mixture was stirred at 20°C for 16 h. The reaction mixture was poured into sat.aq.NH4Cl (50 mL). The aqueous phase was extracted with ethyl acetate (50 mL x 3). The combined organic phase was washed with brine (50 mL), dried with anhydrous Na ₂ SO ₄ , filtered and concentrated in vacuum. The residue was purified by flash silica gel chromatography (ISCO®; 40 g SepaFlash® Silica Flash Column, Eluent of 0~40% Ethyl acetate/Petroleum ethergradient @ 40 mL/min) to give [2-formyl-4-(3-pyridyl)phenyl] trifluoromethanesulfonate (4 g, 12.0mmol, 60.1% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.35 (s, 1H), 8.87 (d, J = 2.4 Hz, 1H), 8.69 (d, J = 4.4 Hz, 1H), 8.20 (d, J = 2.4 Hz, 1H), 7.96-7.91 (m, 2H), 7.55 (d, J = 8.4 Hz, 1H), 7.46 (dd, J = 8.0, 4.8 Hz, 1H). [0603] F23.4 Preparation of 5-(3-pyridyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan- 2-yl) benzaldehyde [0604] To a mixture of [2-formyl-4-(3-pyridyl)phenyl] trifluoromethanesulfonate (1.50 g, 4.53 mmol, 1 eq) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborola n-2-yl)-1,3,2- dioxaborolane (1.72 g, 6.79 mmol, 1.5 eq) in dioxane (15 mL) was added Pd(dppf)Cl ₂ (166 mg, 226 umol, 0.05 eq) and KOAc (1.11 g, 11.3 mmol, 2.5 eq) at 25°C under N ₂ . The mixture was stirred at 80°C for 16 h. The reaction mixture was cooled to r.t. and filtered through a pad of celite. The filtrate was concentrated under reduced pressure to give a residue. The residue was purified by flash silica gel chromatography (ISCO®; 20 g SepaFlash® Silica Flash Column, Eluent of 0~40% Ethyl acetate/Petroleum ethergradient @ 20 mL/min) to give 5-(3-pyridyl)-2- (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzaldehyde (0.900 g, 2.91 mmol, 64.3% yield) as yellow oil. ¹ H NMR (CDCl ₃ , 400 MHz) δ 10.67 (s, 1H), 8.89 (s , 1H), 8.64 (d, J = 4.8 Hz, 1H), 8.20 (d, J = 1.6 Hz, 1H), 8.02 (d, J = 8.0 Hz, 1H), 7.97-7.92 (m, 1H), 7.83 (d, J = 8.0 Hz, 1H), 7.41 (dd, J = 7.6, 5.2 Hz, 1H), 1.41 (s, 1 ₂ H). [0605] F23.5 Preparation of (2-chlorophenyl)-[1-hydroxy-6-(3-pyridyl)-2,3,1- benzodiazaborinin- 2-yl]methanone [0606] To a mixture of 5-(3-pyridyl)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2- yl)benzaldehyde (300 mg, 970 umol, 1 eq) and 2-chlorobenzohydrazide (166 mg, 970 umol, 1 eq) in EtOH (3.5 mL) and NH ₃ .H ₂ O (0.3 mL, 25% purity) at 20°C. The mixture was stirred at 50°C for 1 h. The mixture was cooled to 20°C and added ice-water (0.2 mL). The resulting solution was purified by prep-HPLC (column: Waters Xbridge Prep OBD C18 150*40mm*10um;mobile phase: [water(0.05%NH ₃ H ₂ O+10mM NH ₄ HCO ₃ )-ACN];B%: 15%- 55%,8min) to give (2-chlorophenyl)-[1-hydroxy-6-(3-pyridyl)-2,3,1-benzodiazabo rinin- 2- yl]methanone (95 mg, 261.13 umol, 26.91% yield, 99.39% purity) as a white solid. ¹ H NMR (DMSO+D2O-d ₆ , 400 MHz) δ 8.90 (s, 1H), 8.56 (s, 1H), 8.21-8.11 (m, 1H), 8.08-7.90 (m, 1H), 7.76 (br s, 1H), 7.76 (br s, 1H), 7.53-7.51 (m, 3H), 7.43-7.36 (m, 3H). MS (ESI): mass calcd. For C ₁₉ H ₁₃ BClN ₃ O ₂ 361.08, m/z found 362.2 [M+H] ⁺ . HPLC: 99.38% (220 nm), 99.94% (254 nm). [0607] F24 Preparation of [4-chloro-2-[(Z)-[(6-chloropyridine-2- carbonyl)hydrazono]methyl] phenyl]boronic acid [0608] F24.1 Preparation of 6-chloropyridine-2-carbohydrazide [0609] To a solution of methyl 6-chloropyridine-2-carboxylate (2.00 g, 11.66 mmol, 1 eq) in MeOH (20 mL) was added N ₂ H ₄ .H ₂ O (715 mg, 13.99 mmol, 694 uL, 98% purity, 1.2 eq) at 20°C. The mixture was stirred at 20°C for 4 h. The reaction mixture was concentrated under reduced pressure to remove MeOH. The residue was triturated with MTBE at 20 ^o C for 10 min. The result suspension was filtered and the filter cake was washed with MTBE (5 mL x 3) to give 6-chloropyridine-2-carbohydrazide (1.00 g, 5.83 mmol, 50.00% yield) as a white solid. ¹ H NMR (CDCl ₃ , 400 MHz) δ 9.03 (br s, 1H), 8.06 (d, J = 7.6 Hz, 1H), 7.81 (t, J = 7.6 Hz, 1H), 7.46 (d, J = 7.6 Hz, 1H), 4.16 (d, J = 4.4 Hz, ₂ H). [0610] F24.2 Preparation of [4-chloro-2-[(Z)-[(6-chloropyridine-2- carbonyl)hydrazono]methyl] phenyl]boronic acid [0611] A mixture of (4-chloro-2-formyl-phenyl)boronic acid (200 mg, 1.08 mmol, 1 eq) and 6-chloropyridine-2-carbohydrazide (205 mg, 1.19 mmol, 1.1 eq) in EtOH (10 mL) was stirred at 20°C for 2 h under N ₂ atmosphere. The reaction mixture was filtered. The filter cake was washed with EtOH (5 mL x 3) and then dried in vacuo to give [4-chloro-2-[(Z)- [(6- chloropyridine-2 -carbonyl)hydrazono]methyl]phenyl]boronic acid (185 mg, 547.41 umol, 50.47% yield) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 12.24 (s, 1H), 8.96 (s, 1H), 8.52 (br s, 2H), 8.11-8.09 (m, ₂ H), 7.93 (d, J = 2.0 Hz, 1H), 7.80 (dd, J = 2.0 Hz, 8.0 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 7.46 (dd, J = 2.0 Hz, 8.0 Hz, 1H). MS (ESI): mass calcd. For C13H10BCl ₂ N3O3, 337.02, m/z found 336.0 [M-H]-. HPLC: N/A (220 nm), N/A (254 nm). [0612] F25 Preparation of [2-[(Z)-[(6-chloropyridine-2- carbonyl)hydrazono]methyl]phenyl] boronic acid [0613] To a solution of (2-formylphenyl)boronic acid (162 mg, 1.08 mmol, 1 eq) in EtOH (10 mL) was added 6-chloropyridine-2-carbohydrazide (204 mg, 1.19 mmol, 1.1 eq) in one portion, then the mixture was stirred at 20°C for 2 h under N ₂ atmosphere. The reaction mixture was filtered. The filter cake was washed with EtOH (5 mL x 3) and dried in vacuo to give [2-[(Z)-[(6-chloropyridine-2-carbonyl)hydrazono]methyl]pheny l]boronic acid (101 mg, 332.78 umol, 30.81% yield) as a white solid. ¹ H NMR (DMSO-d6, 400 MHz) δ 12.10 (s, 1H), 8.94 (s, 1H), 8.49 (br s, ₂ H), 8.12-8.09 (m, ₂ H), 7.92 (d, J = 7.2 Hz, 1H), 7.79 (dd, J = 1.6 Hz, 8.0 Hz, 1H), 7.63 (d, J = 7.2 Hz, 1H), 7.46 -7.39 (m, 2H). MS (ESI): mass calcd. For C13H11BClN3O3, 303.06, m/z found 302.0 [M-H]-. HPLC: N/A (220 nm), N/A (254 nm). [0614] Compounds may be made as herein described, for example, according to one or more of the General Procedures F-A or F-B and are characterized as follows in Table 1:

Atty Ref No 81826-321221_BOR-112-PCT [0615] Section II: Biological Materials and Methods [0616] Biological Example 1. Fungal isolates [0617] The isolates of Botrytis cinerea B16, Botrytis cinerea B17, Candida albicans was obtained from the Plant Pathology and Environmental Microbiology Department at The Pennsylvania State University, University Park, PA. The Alternaria linariae isolate was kindly gifted by Inga Meadows at The Department of Entomology and Plant Pathology, Mountain Research Station in North Carolina State University, Waynesville, NC. The Alternaria solani isolate was kindly gifted by Dr. Noah Rosenzweig at The Department of Plant, Soil, and Microbial Sciences, Michigan State University, East Lansing, MI. The isolates of Botrytis cinerea B05.10, Fusarium oxysporum f. sp. cubense TR4, and Phytophthora capsici were obtained from the Texas A&M Agrilife Research, College Station, TX. The isolate of Zymoseptoria triticii CBS100329 was obtained from the Westerdijk Fungal Biodiversity Institute, Utrecht, Netherlands. The isolate of Phytophthora capcisi P1091 was obtained from American Type Culture Collection (ATCC), Manassas, VA. isolate of Podosphaera xanthii was obtained from Dr. Lina Quesada-Ocampo at the Department of Entomology and Plant Pathology at North Carolina State University, Raleigh, NC. The isolates of Sclerotinia sclerotiorum 1980 were obtained from Dr. Jim Steadman at University of Nebraska-Lincoln, Lincoln, NE. The isolate of Phakopsora pachyrhizi isolate was kindly gifted by Dr. Boyd Padgett at the Department of Plant Pathology and Crop Physiology, Louisiana Sate University, Baton Rouge, LA. [0618] Biological Example 2. Fungal and inoculum preparation [0619] Unless specified, most of the organisms were maintained on potato dextrose agar (PDA), and spores may be isolated from the cultures after 1-2 weeks of incubation at room temperature (20-22°C) with 12 hours fluorescent light (Philips, F40LW) and 12hours blacklight (Philips, F40T12) photoperiod. The final concentrations of all inocula were 1 x 10 ⁵ CFU/mL. [0620] Rhizoctonia solani: due to insufficient sporulation from these fungi, inoculum was prepared as mycelium visible fragments. In brief, fungal mycelium grown on agar media were cut into 1x1mm pieces and cultured in autoclaved broth medium (such as PDB and V8). After 3-7 days of incubation at 22-24°C, mycelia were harvested by filtering through one layer of Miracloth™ (Merck Millipore). The mycelia were homogenated in half strength of broth medium using household blender for 10 seconds and filtered through one layer of Miracloth™. The resultant visible fragments were diluted in half strength broth medium. [0621] Fusarium oxysporum f. sp. cubense: the isolate of Fusarium oxysporum f. sp. cubense TR4 was maintained on V8 agar (20% - 200 mL V8 juice, 2 g CaCO3, 15 g Agar, 800 mL distilled water. Spore suspensions were prepared in half strength PDB broth medium with 0.1% Tween® 20. [0622] Sclerotinia sclerotiorum: due to insufficient sporulation from these fungi, inoculum was prepared as mycelium visible fragments. In brief, fungal mycelium grown on agar media (PDA) were cut into 1x1mm pieces and cultured in autoclaved broth medium (such as PDB and V8). After 3-7 days of incubation at 22-24°C, mycelia were harvested by filtering through one layer of Miracloth™ (Merck Millipore). The mycelia were homogenated in half strength of broth medium using household blender for 10 seconds and filtered through one layer of Miracloth™. The resultant visible fragments were diluted in half strength broth medium. [0623] Biological Example 3. In vitro antifungal efficacy of boron-based molecules [0624] A number of boron-based compounds were stocked in DMSO with the concentration of 5000 µg/mL (stored at -20°C). The stock solutions were further diluted into sterile half strength broth media in the in vitro assay, in which DMSO final concentration is not greater than 1% (v/v). [0625] The minimal inhibitory concentrations (MICs) for individual compounds were determined by following a modified broth microdilution protocol. The studies were performed in flat bottom, 96-well microtiter plates (Greiner Bio-One™, Greiner Bio-One North America, Inc., Monroe, NC). The individual MICs were determined in triplicate in a final volume of 0.2 mL/well with antifungal concentrations of 0.2 – 25 µg/mL (8 serial dilutions down from 25 µg/mL [25, 12.5, 6.25, 3.13, 1.56, 0.78, 0.39 and 0.20 µg/mL]; control studies with 0 µg/mL of compounds were performed in parallel for each plate). [0626] Plates sealed with clear polyester film (VWR) were incubated at a temperature of about 22°C. The progress of fungal growth was monitored at 72 hours. The MICs were determined as the lowest antifungal concentrations that inhibited fungal growth by greater than 95% (determined as relative absorbance using the Bio-Tek® Synergy™ H1 microplate reader at 600 nm) relative to the corresponding antifungal-free control. When compounds were screened in vitro more than once, the average MIC of all trials is reported. [0627] Tables showing data against various fungi are provided as Figures. [0628] General example for in vivo testing solutions: [0629] For greenhouse and field trial studies compounds were prepared in the following manner. Compound was dissolved in acetone for a concentration of 1 mg/mL. All % are (v/v) based on the final volume of the spray solution. Aqueous phase was prepared by mixing 49.80% deionized water, 0.10% Silwet Stik 2, and 0.10% Silwet L-77 to a homogenous solution. Acetone phase was then prepared by aliquoting 4-50% of compound stock into a vessel and then adding 0-46% to bring the acetone phase to 50% of the total spray solution. The acetone phase was then mixed with the aqueous phase and was then ready for spray application. [0630] Biological Example 4a. Greenhouse Podosphaera xanthii efficacy of boron-based molecules [0631] Two compounds, EXAMPLE 22 and EXAMPLE 51, were screened under greenhouse conditions against powdery mildew of cucurbits. Each compound was tested against 36 plants (3 doses, 4 plants per dose, 3 replications). Fourteen days after emergence of the cucurbit (V2- V3 growth stage), compound solutions were applied at three separate doses: 250, 100, and 50 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (23°C and 60-70% humidity). Inoculum was prepared by growing P. xanthii on live, susceptible cucurbit plants at 23°C. Leaves were harvested and spores were washed off with sterile, distilled water. Spores were then place in a 0.1% Tween 20 (SigmaAldrich, St. Louis, MO) solution. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 100% powdery mildew infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. See Tables 6 and 7 below. [0632] Biological Example 4b. Greenhouse Podosphaera xanthii efficacy of boron-based molecules [0633] Compounds were screened under greenhouse conditions against powdery mildew of cucurbits. Each compound was tested against 36 plants (3 doses, 4 plants per dose, 3 replications). Fourteen days after emergence of the cucurbit (V2-V3 growth stage), compound solutions were applied at three separate doses: 500, 250, and 125 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (23°C and 60-70% humidity). Inoculum was prepared by growing P. xanthii on live, susceptible cucurbit plants at 23°C. Leaves were harvested and spores were washed off with sterile, distilled water. Spores were then place in a 0.1% Tween 20 (SigmaAldrich, St. Louis, MO) solution. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 100% powdery mildew infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. [0634] Table 2 [0635] Biological Example 5a. Greenhouse Botrytis cinerea efficacy of boron-based molecules [0636] Two compounds, EXAMPLE 22 and EXAMPLE 51, were screened under greenhouse conditions against grey mold of tomato. Each compound was tested tested against 36 plants (3 doses, 4 plants per dose, 3 replications). Eighteen days after emergence of the tomato (V2-V3 growth stage), compound solutions were applied at three separate doses: 250, 100, and 50 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (22°C and 90% humidity). Inoculum was prepared by transferring plugs of Botrytis cinerea into sterile potato dextrose broth. After three days,the liquid culture was centrifuged for 10 minutes at 5000 rpm. The supernant was poured off and the spores were resuspend in sterile water amended with 0.01% Tween 20. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 80-90% grey mold infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. See Tables 6 and 7 below. [0637] Biological Example 5b. In vivo Botrytis cinerea efficacy of boron-based molecules [0638] Compounds were screened under greenhouse conditions against grey mold of grape. Each compound was tested tested against 18 grapes (3 doses, 6 grapes per dose). Grapes were sanitized in 10% bleach solution and triple rinsed in ddH2o. Compound solutions were applied at three separate doses: 500, 250, and 125 ppm. Grapes were allowed to dry for 5 hours. Inoculum was prepared by transferring plugs of Botrytis cinerea into sterile potato dextrose broth. After three days,the liquid culture was centrifuged for 10 minutes at 5000 rpm. The supernant was poured off and the spores were resuspend in sterile water amended with 0.01% Tween 20. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each grape was then soaked with the spore suspension. Seven to ten days after inoculation, when the untreated control plants reached 80-90% grey mold infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. [0639] Table 3

[0640] Biological Example 6. Greenhouse Puccinia triticina efficacy of boron-based molecules [0641] Two compounds, EXAMPLE 22 and EXAMPLE 51, were screened under greenhouse conditions against brown rust of wheat. Each compound was tested tested against 36 plants (3 doses, 4 plants per dose, 3 replication). Eighteen days after emergence of the wheat (tillering growth stage), compound solutions were applied at three separate doses: 250, 100, and 50 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (23°C and 70-80% humidity). Inoculum was prepared by growing P. triticina on live, susceptible wheat plants at 16°C. Leaves were harvested and spores was washed off with sterile, distilled water. Spores were then place in a 0.1% Tween 20 (SigmaAldrich, St. Louis, MO) solution. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 60-70% rust infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. See Tables 6 and 7 below. [0642] Biological Example 7a. Greenhouse Alternaria solani efficacy of boron-based molecules [0643] Two compounds, EXAMPLE 22 and EXAMPLE 51, were screened under greenhouse conditions against early blight of tomato. Each compound was tested tested against 36 plants (3 doses, 4 plants per dose, 3 replications). Eighteen days after emergence of the tomato (V2-V3 growth stage), compound solutions were applied at three separate doses: 250, 100, and 50 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (25°C and 90% humidity). Inoculum was prepared by transferring plugs of A. solani into sterile V8 broth. After three days,the liquid culture was centrifuged for 10 minutes at 5000 rpm. The supernatant was poured off and the spores were resuspend in sterile water amended with 0.01% Tween 20. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 80-90% early blight infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. See Tables 6 and 7 below. [0644] Biological Example 7b. Greenhouse Alternaria solani efficacy of boron-based molecules [0645] Compounds were screened under greenhouse conditions against early blight of tomato. Each compound was tested tested against 36 plants (3 doses, 4 plants per dose, 3 replications). Eighteen days after emergence of the tomato (V2-V3 growth stage), compound solutions were applied at three separate doses: 500, 250, and 125 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (25°C and 90% humidity). Inoculum was prepared by transferring plugs of A. solani into sterile V8 broth. After three days,the liquid culture was centrifuged for 10 minutes at 5000 rpm. The supernatant was poured off and the spores were resuspended in sterile water amended with 0.01% Tween 20. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 80-90% early blight infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. [0646] Table 4

[0647] Biological Example 8. Greenhouse Phakopsora pachirhyzi efficacy of boron-based molecules [0648] Compounds were screened under greenhouse conditions against Asian soybean rust. Each compound was tested tested against 36 plants (3 doses, 4 plants per dose, 3 replication). Fourteen days after emergence of the soybean (V2-V3 growth stage), compound solutions were applied at three separate doses: 500, 250, and 125 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (28°C and 90% humidity). Inoculum was prepared by growing P. pachirhyzi on live, susceptible soybean plants at 28°C. Leaves were harvested and spores was washed off with sterile, distilled water. Spores were then place in a 0.1% Tween 20 (SigmaAldrich, St. Louis, MO) solution. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Ten to fourteen days after inoculation, when the untreated control plants reached 80-90% rust infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. [0649] Table 5 [0650] Biological Example 9. Greenhouse Zymoseptoria triticii efficacy of boron-based molecules [0651] Two compounds, EXAMPLE 22 and EXAMPLE 51, were screened under greenhouse house conditions against Septoria leaf blotch of wheat. Each compound was tested tested against 36 plants (3 doses, 4 plants per dose, 3 replication). Eighteen days after emergence of the wheat (tillering growth stage), compound solutions were applied at three separate doses: 250, 100, and 50 ppm. Plants were allowed to dry for 24 hours. After 24 hours, plants were moved into a greenhouse room with optimal conditions for infection (20°C and 90% humidity). Inoculum was prepared by transferring plugs of Z. triticii into sterile yeast sugar broth. After three days,the liquid culture was centrifuged for 10 minutes at 5000 rpm. The supernant was poured off and the spores were resuspend in sterile water amended with 0.01% Tween 20. Spore concentrations were adjusted to 1 x 10 ⁶ cfu/mL. Each plant was then soaked with the spore suspension. Fourteen to twenty days after inoculation, when the untreated control plants reached 70-80% leaf blotch infection, disease ratings were taken and each plant was given a percent infection score. All data were reported and percent disease control compared to the untreated control plants. [0652] Table 6 [0653] Table - 7: Percent disease control 1 7 [0654] As demonstrated the compounds of the present invention demonstrate activity and, in some cases exceptional activity, as disease control agents. [0655] Biological Example 10a. In-field Puccinia polysora efficacy of boron-based molecules [0656] Corn was planted into two-row by 15-ft plots (~6-in between plants to give a target population of 60 plants/plot at 36-in row spacing) replicated three times in a randomized complete block design.11 treatments (including a untreated control) were tested for efficacy in managing Southern Corn Rust cause by Puccinia polysora. The first foliar application of treatments was applied when the plants reached growth stage V6 (28 days after planting (DAP)). A second foliar application was applied at VT (49 DAP). One week after the application of treatments, disease ratings were taken on a seven-day schedule until the untreated control approached 100% infection. At the completion of the growing season, each plot was harvested, and yield was calculated (113 DAP). The treatment list is as follows: [0657] Table 8 -188- [0658] Spray solutions were mixed just prior to spraying each treatment in the appropriate amount of water to achieve a 187 liter per hectare spray rate using a CO2 powered hand boom backpack sprayer. Seven days after the first treatment, disease ratings were taken. Each plot was rated at three locations in the plot; front, middle and back where 10 corn plants were randomly sampled per leaf location. Leaves three through 8 were each given a disease rating. Of the 10 leaves randomly sampled per leaf position and location within the plot a % severity rating (coverage of rust pustules on the leaf surface) was assessed. If the leaf was not present at a canopy position due to defoliation caused by disease, then a rating of 100 was given. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season. Ratings were taken on a seven-day schedule until the completion of the trial. Results are as follows: [0659] Table 9: Southern Corn Rust Area Under Disease Progress Curve (AUDPC) on Leaf 4 showing the total disease throughout the growing season. [0660] *Means followed by the same letter are not significantly different from each other (α=0.05). [0661] Table 10: Southern Corn Rust Area Under Disease Progress Curve (AUDPC) on Leaf 5 showing the total disease throughout the growing season. [0662] *Means followed by the same letter are not significantly different from each other (α=0.05). [0663] Table 11: Southern Corn Rust Area Under Disease Progress Curve (AUDPC) on Leaf 6 showing the total disease throughout the growing season. [0664] *Means followed by the same letter are not significantly different from each other (α=0.05). [0665] Table 12: Southern Corn Rust Yield Data—113 days after planting and 72 days after the second fungicide application [0666] *Means followed by the same letter are not significantly different from each other (α=0.05). [0667] Biological Example 10b. In-field Cochliobolus heterostrophus efficacy of boron- based molecules [0668] Corn was planted into two-row by 15-ft plots (~6-in between plants to give a target population of 60 plants/plot at 36-in row spacing) replicated three times in a randomized complete block design.11 treatments (including a untreated control) were tested for efficacy in managing Southern Corn Leaf Blight caused by Cochliobulus heterostrophus. Field trial pathogens included Ascomycota or Basidiomycota. The first foliar application of treatments was applied when the plants reached growth stage V6 (28 days after planting (DAP)). A second foliar application was applied at VT (49 DAP). One week after the application of treatments, disease ratings were taken on a seven-day schedule until the untreated control approached 100% infection. At the completion of the growing season, each plot was harvested, and yield was calculated (113 DAP). The treatment list is as follows: [0669] Table 13 [0670] Spray solutions were mixed just prior to spraying each treatment in the appropriate amount of water to achieve a 187 liter per hectare spray rate using a CO ₂ powered hand boom backpack sprayer. Seven days after the first treatment, disease ratings were taken. Each plot was rated at three locations in the plot; front, middle and back where 10 corn plants were randomly sampled per leaf location. Leaves three through 8 were each given a disease rating. Of the 10 leaves randomly sampled per leaf position and location within the plot a % severity rating (coverage of SCLB lesions on the leaf surface) was assessed. If the leaf was not present at a canopy position due to defoliation caused by disease, then a rating of 100 was given. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season. Ratings were taken on a seven-day schedule until the completion of the trial. Results are as follows: [0671] Table 14: Southern Corn Leaf Blight Area Under Disease Progress Curve (AUDPC) on Leaf 4 showing the total disease throughout the growing season. [0672] *Means followed by the same letter are not significantly different from each other (α=0.05). [0673] Table 15: Southern Corn Leaf Blight Area Under Disease Progress Curve (AUDPC) on Leaf 5 showing the total disease throughout the growing season. [0674] *Means followed by the same letter are not significantly different from each other (α=0.05). [0675] Table 16: Southern Corn Leaf Blight Area Under Disease Progress Curve (AUDPC) on Leaf 6 showing the total disease throughout the growing season. [0676] *Means followed by the same letter are not significantly different from each other (α=0.05). [0677] Table 17: November 29 Southern Corn Leaf Blight Yield Data—113 days after planting and 72 days after the second fungicide application -194- [0678] *Means followed by the same letter are not significantly different from each other (α=0.05). [0679] Biological Example 11. In-field Podosphaera xanthii efficacy of boron-based molecules [0680] Yellow crookneck squash was planted into one-row by 16-ft plots (~12-in between plants to give a target population of 16 plants/plot at 72-in row spacing) replicated three times in a randomized complete block design. Nineteen treatments (including an untreated control) were tested for efficacy in managing cucurbit powdery mildew cause by Podosphaera xanthii. The first foliar application of treatments was applied on October 30, 35 days after transplanting and subsequent applications were applied on a 7-day schedule until November 13 for a total of 3 applications. An initial disease rating was taken on November 1, two days after the first application. Subsequent disease ratings were taken every 4 days until the conclusion of the trial. The treatment list is as follows: [0681] Table 18 [0682] Spray solutions were mixed just prior to spraying each treatment in the appropriate amount of water to achieve a 375 liter per hectare spray rate using a CO2 powered hand boom backpack sprayer. Two days after the first treatment, disease ratings were taken. Each plot was rated at three locations in the plot; front, middle and back where 2 plants where given a rating on the lower, middle, and upper canopy. Each canopy position was given a % severity rating (coverage of powdery mildew on the leaf surface). If the leaf was not present at a canopy position due to defoliation caused by disease, then a rating of 100 was given. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season for the lower, middle, and upper canopy. Ratings were taken on a four-day schedule until the completion of the trial. Results are as follows: [0683] Table 19: Cucurbit Powdery Mildew Area Under Disease Progress Curve (AUDPC) in the Lower Canopy showing the total disease throughout the growing season. [0684] *Means followed by the same letter are not significantly different from each other (α=0.05). [0685] Table 20: Cucurbit Powdery Mildew Area Under Disease Progress Curve (AUDPC) in the Middle Canopy showing the total disease throughout the growing season. [0686] *Means followed by the same letter are not significantly different from each other (α=0.05). [0687] Table 21: Cucurbit Powdery Mildew Area Under Disease Progress Curve (AUDPC) in the Upper Canopy showing the total disease throughout the growing season. [0688] *Means followed by the same letter are not significantly different from each other (α=0.05). [0689] Biological Example 12. In-Field Phakopsora pachyrhizi efficacy of boron-based molecules. [0690] Soybeans were planted into two-row by 30-ft plots (~7-in. between plants to give a target population of 100 plants/plot at 36-in. row spacing) replicated four times in a randomized complete block design. Six treatments (including an untreated control) were tested for efficacy in managing Asian soybean rust (ASR) caused by Phakopsora pachyrhizi. The first foliar application of treatments was applied when the soybean beans reached growth stage V5. An initial disease rating was taken 20 days after the first foliar application. Subsequent disease ratings were taken every seven days until the untreated control approached 100% infection. A second and third foliar application of treatment was applied at growth stage R1 and R3. At the completion of the growing season, each plot was harvested, and yield was calculated.This trial was replicated once at the same location in a separate area of of the research station. [0691] Each plot was rated at three locations: front, middle and back; 10 leaves of soybean were randomly sampled per canopy location. The locations selected in the canopy were defined as lower, middle and upper leaves. Of the 10 leaves randomly sampled per canopy position and location within the plot, a % severity rating (infection of ASR on the leaf surface) was assessed. If the leaf was not present at a canopy position due to defoliation caused by ASR, then a number of 100% was given. Additionally, ratings were taken for frogeye leaf spot (FLS) caused by Cercospora sojina as it naturally infested the trial towards the end of the season. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season. Results are as follows: [0692] Table 22: Asian Soybean Rust Area Under Disease Progress Curve (AUDPC) of the Lower Canopy showing the total disease throughout the growing season. [0693] *Means followed by the same letter are not significantly different from each other (α=0.05). [0694] Table 23: Asian Soybean Rust Area Under Disease Progress Curve (AUDPC) of the Middle Canopy showing the total disease throughout the growing season. [0695] *Means followed by the same letter are not significantly different from each other (α=0.05). [0696] Table 24: Asian Soybean Rust Area Under Disease Progress Curve (AUDPC) of the Upper Canopy showing the total disease throughout the growing season.

[0697] *Means followed by the same letter are not significantly different from each other (α=0.05). [0698] Table 25: Frogeye Leaf Spot Area Under Disease Progress Curve (AUDPC) of the Upper Canopy showing the total disease throughout the growing season. [0699] *Means followed by the same letter are not significantly different from each other (α=0.05). [0700] Table 26: Asian Soybean Rust Yield Data—124 days after planting and 76 days after the final fungicide application. -200- [0701] *Means followed by the same letter are not significantly different from each other (α=0.05). [0702] SECOND TRIAL [0703] Table 27: Asian Soybean Rust Area Under Disease Progress Curve (AUDPC) of the Lower Canopy showing the total disease throughout the growing season. [0704] *Means followed by the same letter are not significantly different from each other (α=0.05). [0705] Table 28: Asian Soybean Rust Area Under Disease Progress Curve (AUDPC) of the Middle Canopy showing the total disease throughout the growing season. [0706] *Means followed by the same letter are not significantly different from each other (α=0.05). [0707] Table 29: Asian Soybean Rust Area Under Disease Progress Curve (AUDPC) of the Upper Canopy showing the total disease throughout the growing season. [0708] *Means followed by the same letter are not significantly different from each other (α=0.05). [0709] Table 30: Asian Soybean Rust Yield Data—129 days after planting and 76 days after the final fungicide application. [0710] *Means followed by the same letter are not significantly different from each other (α=0.05). [0711] Biological Example 13. In-field Puccinia polysora efficacy of boron-based molecules [0712] Maize was planted into two-row by 15-ft plots (~6-in between plants to give a target population of 60 plants/plot at 36-in row spacing) replicated four times in a randomized complete block design. Six treatments (including an untreated control) were tested for efficacy in managing southern corn rust caused by Puccinia polysora. The first foliar application of treatments was applied when the plants reached growth stage V6. A second foliar application was applied at R1. One week after the application of treatments, disease ratings were taken on a seven-day schedule until the untreated control approached 100% infection. At the completion of the growing season, each plot was harvested, and yield was calculated. [0713] Three days after the first treatment, disease ratings were taken. Each plot was rated at three locations in the plot, front, middle and back, where 10 corn plants were randomly sampled per leaf location. Leaves three through eight were each given a disease rating. Of the 10 leaves randomly sampled per leaf position and location within the plot, a % severity rating (coverage of rust pustules on the leaf surface) was assessed. If the leaf was not present at a canopy position due to defoliation caused by disease, then a rating of 100 was given. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season. Results are as follows: [0714] Table 31: Southern Corn Rust Area Under Disease Progress Curve (AUDPC) on Leaf 4 showing the total disease throughout the growing season. [0715] *Means followed by the same letter are not significantly different from each other (α=0.05). [0716] Table 32: Southern Corn Rust Area Under Disease Progress Curve (AUDPC) on Leaf 5 showing the total disease throughout the growing season.

[0717] *Means followed by the same letter are not significantly different from each other (α=0.05). [0718] Table 33: Southern Corn Rust Area Under Disease Progress Curve (AUDPC) on Leaf 6 showing the total disease throughout the growing season. [0719] *Means followed by the same letter are not significantly different from each other (α=0.05). [0720] Table 34 Southern Corn Rust Yield Data—131 days after planting and 76 days after the second fungicide application. -204- [0721] *Means followed by the same letter are not significantly different from each other (α=0.05). [0722] Biological Example 14. In-field Cochliobolus heterostrophus efficacy of boron- based molecules [0723] Maize was planted into two-row by 15-ft plots (~6-in between plants to give a target population of 60 plants/plot at 36-in row spacing) replicated four times in a randomized complete block design. Six treatments (including an untreated control) were tested for efficacy in managing southern corn leaf blight caused by Cochliobolus heterostrophus. The first foliar application of treatments was applied when the plants reached growth stage V6. A second foliar application was applied at R1. One week after the application of treatments, disease ratings were taken on a seven-day schedule until the untreated control approached 100% infection. At the completion of the growing season, each plot was harvested, and yield was calculated. [0724] Three days after the first treatment, disease ratings were taken. Each plot was rated at three locations in the plot, front, middle and back, where 10 corn plants were randomly sampled per leaf location. Leaves three through six were each given a disease rating. Of the 10 leaves randomly sampled per leaf position and location within the plot, a % severity rating (coverage of SCLB lesions on the leaf surface) was assessed. If the leaf was not present at a canopy position due to defoliation caused by disease, then a rating of 100 was given. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season. Results are as follows: [0725] Table 35: Southern Corn Leaf Blight Area Under Disease Progress Curve (AUDPC) on Leaf 4 showing the total disease throughout the growing season.

[0726] *Means followed by the same letter are not significantly different from each other (α=0.05). [0727] Table 36: Southern Corn Leaf Blight Area Under Disease Progress Curve (AUDPC) on Leaf 5 showing the total disease throughout the growing season. [0728] *Means followed by the same letter are not significantly different from each other (α=0.05). [0729] Table 37: Southern Corn Leaf Blight Area Under Disease Progress Curve (AUDPC) on Leaf 6 showing the total disease throughout the growing season. [0730] *Means followed by the same letter are not significantly different from each other (α=0.05). [0731] Table 38: Southern Corn Leaf Blight Yield Data—131 days after planting and 76 days after the second fungicide application. [0732] *Means followed by the same letter are not significantly different from each other (α=0.05). [0733] Biological Example 15. In-field Podosphaera xanthii efficacy of boron-based molecules [0734] Yellow crookneck squash was planted into one-row by 30-ft plots (~16-in between plants to give a target population of 22 plants/plot at 72-in row spacing) replicated three times in a randomized complete block design. Six treatments (including an untreated control) were tested for efficacy in managing cucurbit powdery mildew cause by Podosphaera xanthii. The first foliar application of treatments was applied 32 days after transplanting and subsequent applications were applied on a 7-day schedule for a total of 4 applications. An initial disease rating was taken five days after the first application. Subsequent disease ratings were taken every 7-14 days until the conclusion of the trial. [0735] Five days after the first treatment, disease ratings were taken. Each plot was rated at three locations in the plot, front, middle and back, where 2 plants where given a rating on the lower, middle, and upper canopy. Each canopy position was given a % severity rating (coverage of powdery mildew on the leaf surface). If the leaf was not present at a canopy position due to defoliation caused by disease, then a rating of 100 was given. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Ratings were taken on a four-day schedule until the completion of the trial. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season for the lower, middle, and upper canopy. Results are as follows: [0736] Table 39: Cucurbit Powdery Mildew Area Under Disease Progress Curve (AUDPC) in the Lower Canopy showing the total disease throughout the growing season. [0737] *Means followed by the same letter are not significantly different from each other (α=0.05). [0738] Table 40: Cucurbit Powdery Mildew Area Under Disease Progress Curve (AUDPC) in the Middle Canopy showing the total disease throughout the growing season. -208- [0739] *Means followed by the same letter are not significantly different from each other (α=0.05). [0740] Table 41: Cucurbit Powdery Mildew Area Under Disease Progress Curve (AUDPC) in the Upper Canopy showing the total disease throughout the growing season. [0741] *Means followed by the same letter are not significantly different from each other (α=0.05). [0742] Biological Example 16. In-field Alternaria solani efficacy of boron-based molecules [0743] Tomatoes were planted into one-row by 30-ft plots (30 plants per plot) replicated four times in a randomized complete block design. Six treatments (including untreated control) were tested for efficacy in managing tomato early blight (TomEB) caused by Alternaria solani. The first foliar application of treatments was applied 59 days after planting when tomatoes reached P-Day 300. The P-Day value represents this physiological age of the tomato plants derived from an algorithm based on air temperature, soil temperature, relative humidity and soil moisture throughout the growing season. Following the initial application, subsequent applications were applied every seven days for a total of five application. Following the initial disease rating subsequent disease ratings were taken every seven days until the conclusion of the trial. [0744] Initial disease ratings were taken to give a baseline for each plot. Early blight severity was assessed for the lower, middle, and upper canopy in the center of each plot using a percent severity rating. Subsequent ratings were taken every seven days. Analysis of variance was used to examine disease severity data and means were separated using Fisher’s least significant difference at α=0.05. Area under disease progress curve (AUDPC) was calculated to show a quantitative summary of disease intensity throughout the growing season. Results are as follows: [0745] Table 42: Tomato Early Blight Area Under Disease Progress Curve (AUDPC) of the Lower Canopy showing the total disease throughout the growing season. [0746] *Means followed by the same letter are not significantly different from each other (α=0.05). [0747] Table 43 Tomato Early Blight Area Under Disease Progress Curve (AUDPC) of the Middle Canopy showing the total disease throughout the growing season. [0748] *Means followed by the same letter are not significantly different from each other (α=0.05). [0749] Table 44: Tomato Early Blight Area Under Disease Progress Curve (AUDPC) of the Upper Canopy showing the total disease throughout the growing season.

[0750] *Means followed by the same letter are not significantly different from each other (α=0.05). [0751] Biological Example 17. In vitro antibacterial efficacy of boron-based molecules [0752] A number of boron-based compounds were stocked in DMSO with the concentration of 5000 µg/mL (stored at -20°C). The stock solutions were further diluted into sterile half strength broth media in the in vitro assay, in which DMSO final concentration is not greater than 1% (v/v). [0753] Escherichia coli (E. coli) and Agrobacterium tumefaciens (A. tumefaciens) were used in antibacterial screening using a test compound of the present disclosure as a potential antibiotic. The final concentration of bacteria in each well was 0.001 OD600. [0754] The inhibition amounts (%) for individual compounds were determined by following a modified broth microdilution protocol. The studies were performed in flat bottom, 96-well microtiter plates (Greiner Bio-One). The individual inhibition rates were determined in triplicate in a final volume of 0.2 mL/well with antibacterial concentration of 25 µg/mL; control studies with 0 µg/mL of compounds were performed in parallel for each plate). [0755] Plates sealed with clear polyester film (VWR) were incubated at a temperature of about 22°C. The progress of bacterial growth was monitored at 48 hours. The inhibition rates were determined using the following formula: inhibition rate % = (OD600 of Control- OD600 of compound)/OD600 of Control * 100. (determined as relative absorbance using the Bio-Tek® Synergy™ H1 microplate reader at 600 nm) relative to the corresponding control. [0756] The results of those studies shown above indicate that compounds of the present disclosure have at best weak antibiotic activity as was reported in Kanichar et al., Chem Biodivers 11:1381-1397 (2014) for those and similar compounds. [0757] Table 45a

[0758] Table 45b MIC95: E. MIC95: B. coli subtilis Compound 24hr_ppm 24hr_ppm [0759] Biological Example 18: In vitro nematicidal efficacy of boron-based molecules on C. elegans [0760] The boron-based molecules were subjected to the high-throughput screening of nematicidal compounds protocol detailed below. [0761] Preparing Buffers [0762] LB broth [0763] LB growth medium(for1liter) 10g bio-tryptone,5g yeast extract,10g NaCl, make up to 1 liter with ddH2O, adjust pH to 7.0, autoclave. [0764] Nematode Growth Medium (NGM) Agar [0765] Mix 23 g of agar, 3 g of NaCl, 2.5 g of bacto peptone, and deionized water to 0.972 L. Autoclave and let cool to 60 °C, then add 25 mL of 1 M potassium phosphate (KPO4) buffer (pH 6.0), 1 mL of 1 M magnesium sulfate (MgSO4), 1 mL of 1 M calcium chloride (CaCl ₂ ), and 1 mL of 5 mg/mL cholesterol (in ethanol). [0766] Hypochlorite solution [0767] 4 ml 10% NaOCl bleach solution, 10 ml 1M NaOH, 4 ml ddH ₂ O. [0768] Potassium citrate pH 6.0 [0769] Mix 20 g citric acid monohydrate, 293.5 g tri-potassium citrate monohydrate, H2O to 1 litre. Sterilize by autoclaving. [0770] Trace metals solution [0771] 1.86 g disodium EDTA, 0.69 g FeSO4 •7 H ₂ O, 0.2 g MnCl ₂ •4 H ₂ O, 0.29 g ZnSO4 •7 H ₂ O, 0.025 g CuSO ₄ •5 H ₂ O, H ₂ O to 1 liter. Sterilize by autoclaving. Store in the dark. [0772] S Basal [0773] Mix 5 g of NaCl, 1 g of K ₂ HPO4, 6 g of KH2PO4, and de-ionized water to 1 L, then autoclave. [0774] S Medium [0775] 1 litre S Basal, 10 ml 1 M potassium citrate pH 6, 10 ml trace metals solution, 3 ml 1 M CaCl ₂ , 3 ml 1 M MgSO ₄ . Add components using sterile technique; do not autoclave.

[0776] M9 Buffer [0777] 3 g KH2PO4, 6 g Na ₂ HPO4, 5 g NaCl, 1 ml 1 M MgSO4, H ₂ O to 1 litre. Sterilize by autoclaving. [0778] MYOB dry mix (for 370 g) [0779] 27.5 g Trizma® HCl (TRIS HCl), 12 g Trizma® base, 230 g bacto tryptone, 100 g NaCl, 0.4 g cholesterol (95%), mix with shaking. [0780] MYOB medium (for 1 liter) [0781] 7.4g MYOB dry mix, 22g agar, make up to1liter with ddH2O, autoclave. [0782] Preparation of Bacterial Food Source (Concentrated E. coli Strain OP50) [0783] Inoculate 2 mL of autoclaved LB broth with a single colony of E. coli (Strain OP50) and incubate for 4-6 hours at 37 °C with shaking at 250 rpm. Use 0.5 mL of this solution to inoculate 0.5 L of LB in a 1 L Erlenmeyer flask (2 flasks). Incubate for 14 hours (overnight) at 37 °C with shaking at 250 rpm. [0784] Centrifuge 1 L overnight cultures in 500 mL centrifuge bottles for 5 minutes at 10,000 x g and 4 °C to pellet the bacteria and decant away remaining media. Resuspend pellet in 25 mL of S Basal. Store at 4 °C. [0785] Preparation of NGM Petri Plates [0786] Mix 3 g NaCl, 17 g agar, and 2.5 g peptone in a 2 liter Erlenmeyer flask. Add 975 ml H ₂ O. Cover mouth of flask with aluminium foil. Autoclave for 50 minutes. [0787] Cool flask in 55°C water bath for 15 minutes. Add 1 ml 1 M CaCl ₂ , 1 ml 5 mg/ml cholesterol in ethanol, 1 ml 1 M MgSO4 and 25 ml 1 M KPO4 buffer. Swirl to mix well. [0788] Using sterile procedures, dispense the NGM solution into petri plates using a peristaltic pump. Fill plates 2/3 full of agar. [0789] Leave plates at room temperature for 2-3 days before use to allow for detection of contaminants, and to allow excess moisture to evaporate. Plates stored in an air-tight container at room temperature are usable for several weeks. [0790] Preparation of C. Elegans Mass Cultures [0791] Add 250 ml S Medium to a sterilized 1-2 liter flask. [0792] Inoculate the S Medium with a concentrated E. coli OP50 pellet made from 2-3 litres of an overnight culture. [0793] Wash each of 4 large plates of C. elegans (just cleared of bacteria) with 5 ml S Medium and add to the 250 ml flask. [0794] Put the flask on a shaker at 20°C. Use fairly vigorous shaking so that the culture is well oxygenated. [0795] Cultures should be monitored by checking a drop of the culture under the microscope. If the food supply is depleted (the solution is no longer visibly cloudy) add more concentrated E. coli OP50 suspended in S Medium. When there are many adult worms in each drop, the culture is ready to be harvested. This is usually on the 4th or 5th day. [0796] Put the flask on ice for 15 minutes to allow the worms to settle. [0797] Aspirate most of the liquid from the flask. [0798] Transfer the remaining liquid to a 50 ml sterile conical centrifuge tube and spin for at least 2 min at 1150 × g to pellet the worms. Young larvae may take longer than 2 minutes to pellet. [0799] Aspirate the remaining liquid. [0800] Preparation of C. elegans Eggs [0801] Add 10 mL hypochlorite solution to the egg pellet and vigorously shake the tube. Incubate 1-3 minutes, with occasional shaking, and while monitoring appearance with the dissecting microscope. Visually confirm only eggs are remaining and proceed to the next step. [0802] Spin down the tube at 1,000 x g for 1.5 min and aspirate off the supernatant. The pellet should be white with no brown coloration. [0803] Wash the pellet 3 times with S basal, spinning down (1,000 x g for 1.5 minutes) and aspirating away the supernatant each time. Re-suspend the egg pellet in 2-3 mL S basal. These eggs may now be used for an overnight hatch in buffer to collect L1 larva. [0804] Preparation of L1 Larval C. elegans [0805] Aseptically transfer the axenized eggs to 250 ml M9 Buffer in a 1-2 liter flask and allow to incubate overnight at 20°C using fairly vigorous shaking to obtained starved L1 animals. [0806] Collect L1s in a 15 mL tube with a serological pipette. Spin down L1s in a centrifuge (1,000 x g for 1.5 minutes), aspirate away the supernatant. [0807] Dilute L1s in S medium to 3 L1s per µL. [0808] 24 -Well Assay Plate Setup [0809] Prepare 1 liter of MYOB medium in a 2-liter flask. [0810] After autoclaving, allow MYOB medium to cool for 1 hour in a 601C water bath. [0811] Using a repeater pipette, add 1 ml warm MYOB medium to each well of forty 24-well tissue culture plates. [0812] Add the bioactive small molecule of interest to the media after it has cooled to 60 ^o C. [0813] Allow the assay plates to reach room temperature (2 hour) and then add 5 µL of concentrated OP50 to each well. [0814] Add 10 µL of L1 suspension to each well. [0815] Dry plates in the laminar flow cabinet for 4-8 hours. [0816] Cover plate with lid and incubate at 25 °C for 3-7 days. [0817] Scoring C. elegans Cultures for mortality [0818] Monitor negative control wells until >95% mortality is observed (about 4 days). [0819] Count and record the number of alive and dead animals in each well. [0820] Inhibition rate is scored by the formula: inhibition rate % = dead animal in the well with compounds/(alive + live animals in the well with compounds)*100 - dead animal in the negative control well/(alive + live animals in the negative control well)*100. [0821] Biological Example 14: Plant parasitic nematode in vitro screening assay [0822] To determine the efficacy of the boron-based molecules, the boron-based molecules were subjected to the in vitro screening assay detailed below. [0823] Plant parasitic nematode culture: The isolate of Heterodera glycines race 3 (soybean cyst nematode) was obtained from Dr. Senyu Chen, University of Minnesota, Waseca, MN. The Meloidogyne incognita (southern root-knot nematode) was obtained from Dr. Ernest Bernard, University of Tennessee, Knoxville, TN. [0824] Nematode inoculum preparation: Nematode eggs were setup for hatching in 4mM ZnCl ₂ solution using modified Baermann tray and incubated in microbiological laboratory incubator at 25 °C. Freshly hatched J2s (second stage juvenile nematode) were collected and disinfected using antibiotic solution (100pp streptomycin, 50ppm chlortetracycline, and 30ppm quinolinol) before use. [0825] In vitro nematicidal efficacy of boron-based molecules: The screening assays were conducted using 48-well microtiter plates. Stock solutions of the chemicals were prepared in dimethyl sulfoxide (DMSO) and distributed into microplates for dilutions (or the same volume of DMSO solution as negative Control). A calculated volume of 1% agarose gel was distributed and mixed with the chemical solutions in each well to complete the testing system by targeted concentration levels at 1ppm, 5ppm, and 25ppm. Leave all plates in room temperature to solidify. Each treatment was set up for four replicates. [0826] An aliquot of nematodes containing approximately 20-30 J2s was distributed onto the surface of the agar plate in each testing well. All screening assays were stored at room temperature. Number of dead J2s were quantified at 24 hours and/or 72 hours after the initial setup.re stored at room temperature. Number of dead J2s were quantified at 24 hours and/or 72 hours after the initial setup. [0827] Statistics: J2 mortality (%) was calculated by (#Dead J2s/ #Total J2s)*100, and then standardized by (%Treatment mortality - %average Control mortality). ANOVA was performed to determine whether there was an overall chemical effect on standardized J2 mortality. Then LSD post hoc test for pairwise comparison (α=0.05) was performed if p-value is smaller than 0.05 in the overall ANOVA test. [0828] In vitro nematicidal efficacy of boron-based molecules [0829] Nematode hatching: [0830] Soybean cyst nematode (SCN, Heterodera glycines) eggs were obtained from Cathy Johnson at the University of Minnesota Southern Research and Outreach Center in Watseca, MN. Root-knot nematode (RKN, Meloidogyne incognita) eggs were obtained from Dr. Gary Lawrence - Plant Diagnostics, LLC in Mt. Airy, NC. Roughly 1,000,000 eggs of each species were hatched by using a modified Baermann funnel described in Pettite et al., 2019. The eggs were placed on two layers of laboratory tissues supported by a wire screen sitting on a Petri dish filled with MilliQ (reverse osmosis, deionized water) water touching the bottom of the screen. This allowed hatched J2s to migrate through the laboratory tissue and fall into the petri dish. After a 48 hour incubation at 30C, J2s of each species were collected into 50mL tubes and transported to the test facility. [0831] Compound preparation: [0832] Boron compounds were prepared as described previously.5mg/mL stocks in DMSO were supplied to in 96 well plates and 1 µL of this stock was dispensed into 100uL of sterile deionized water in column 2 of a new round bottom 96 well plate using a Biomek NX.1:2 dilutions in sterile deionized water were made from column 2 to column 11 as shown below. Negative control wells contained sterile, deionized water and positive control wells contained a mixture of 10ppm fluopyram and 10ppm abamectin. [0833] Assay: [0834] The hatched nematode J2 stocks were quantified via hemacytometer and diluted to 300 J2s/mL and 100uL was aliquoted into each well. Plates were incubated for 48 hours following addition of compounds. Activity was assessed using an LCD camera imaging system to determine nematode motility relative to the average motility of untreated nematodes in control wells containing DMSO with no compound. IDBS XLfit™ software may be used to generate sigmoidal curves for EC50 determination in dose response plates. [0835] Post-processing: [0836] Root-knot nematode data was entered using IDBS XLfit™ software for RKN. Images were evaluated in a similar fashion, using FIJI/ImageJ software to determine the number of motile nematodes in each well and the Schneider-Orelli formula was used to account for control mortality on each plate. Graphpad Prism 8 was used to convert the percent mortality data sets, using nonlinear regression analysis with a [Agonist/Inhibitor vs. normalized response] model, rendering EC50 values. The results of Table 46 were graphed and are depicted on Figure 3. [0837] Table 46

[0839] Although this specification contains many specific implementation details, these should not be construed as limitations on the scope of any disclosure or on the scope of what may be claimed, but rather as descriptions of features that may be specific to particular implementations of particular disclosures. Certain features that are described in this specification in the context of separate implementations may also be implemented in combination in a single implementation. Conversely, various features that are described in the context of a single implementation may also be implemented in multiple implementations separately or in any suitable sub-combination. Moreover, although features may be described above as acting in certain combinations and even initially claimed as such, one or more features from a claimed combination may in some cases be excised from the combination, and the claimed combination may be directed to a sub-combination or variation of a sub-combinations. [0840] Particular implementations of the subject matter have been described. Other implementations, alterations, and permutations of the described implementations are within the scope of the following claims as will be apparent to those skilled in the art. For example, the actions recited in the claims may be performed in a different order and still achieve desirable results. [0841] Accordingly, the above description of example implementations does not define or constrain this disclosure. Other changes, substitutions, and alterations are also possible without departing from the spirit and scope of this disclosure. [0842] A number of embodiments of the present disclosure have been described. Although this specification contains many specific implementation details, the specific implementation details should not be construed as limitations on the scope of any disclosures or of what may be claimed, but rather as descriptions of features specific to particular embodiments of the present disclosure. Nevertheless, it will be understood that various modifications may be made without departing from the spirit and scope of the claimed disclosure.