The control of arthropod pests is extremely important in achieving high crop efficiency.

Arthropod damage to growing and stored agronomic crops can cause significant reduction in productivity and thereby result in increased costs to the consumer. The control of arthropod pests in forestry, greenhouse crops, ornamentals, nursery crops, stored food and fiber products, livestock, household, and public and animal health is also important. The control of plant diseases caused by fungal plant pathogens is also extremely important in achieving high crop efficiency. Plant disease damage to ornamental, vegetable, field, cereal, and fruit crops can cause significant reduction in productivity and thereby result in increased costs to the consumers. Many products are commercially available for these purposes, but the need continues for new compounds which are more effective, less costly, less toxic, environmentally safer or have different modes of action.

WO 96/06086 discloses compounds of Formula i and their composition and method of use as pest control agents R1 is halogen, C2-Cs acyloxy, OH, C1-C4 alkoxy or Cl-C4 alkylthio; and R2 is Cl-C8 alkyl, phenyl, pyrimidinylamino, Cl-C6 alkoxy, COOR3, amino or NHCOR4.

The cyclohexylamines of the present invention are not disclosed in this publication.

SUMMARY OF THE INVENTION This invention is directed to compounds of Formula I including all geometric and stereoisomers, agriculturally suitable salts thereof, agricultural compositions containing them and their use as arthropodicides and fungicides,

wherein: G is selected from the group consisting of Y is a direct bond or C1-C4 alkylene optionally substituted with C1-C4 alkyl; X is O, NR7 or S (O) p; each Z is independently selected from N and CR3; each Z1 is independently selected from O, S and NR8; each R1 is independently selected from the group consisting of H, halogen, C 1-C4 alkyl, Ci-C4 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy and R9S (O) p; each R2 is independently selected from the group consisting of H, CF3, C1 alkyl optionally substituted with one or two R10 substituents, C2-C4 alkyl, R1°CH2CH2-, (R1°) 2CHCH2, R1°CH2CH (Rl°)-, CH3C (R10) 2-, C3-C4 haloalkyl, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl, C1-C4 alkoxy, C1-C4 haloalkoxy, halogen, hydroxy, C2-C4 alkylcarbonyl, C2-C4 haloalkylcarbonyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, cyano, nitro, thiocyanato, C2-C4 alkoxycarbonyl, C2-C4 haloalkoxycarbonyl, C1-C4 alkylamino, C2-C4 dialkylamino and R11S (O) p; each R3 is independently selected from the group consisting of H, C1-C4 alkyl optionally substituted with one or two R10, CF3, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl, C1-C4 alkoxy, C1-C4 haloalkoxy, halogen, hydroxy, C2-C4 alkylcarbonyl, C2-C4 haloalkylcarbonyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, cyano, nitro, thiocyanato,

C2-C4 alkoxycarbonyl, C2-C4 haloalkoxycarbonyl, C1-C4 alkylamino, C2-C4 dialkylamino and R1lS (O) p; or R2 and R3 with the carbon atoms to which they are attached are taken together to form a: (1) 5-or 6-membered unsaturated carbocyclic ring optionally substituted with R12; or (2) 5-or 6-membered unsaturated heterocyclic ring optionally substituted with R12 containing at least one of the atoms selected from O, N and S in the ring; or R2 and R3 with the carbon atoms to which they are attached are taken together to form a: (1) 5-, 6-or 7-membered saturated carbocyclic ring optionally substituted with a C1-C4 alkyl group; or (2) 5-, 6-or 7-membered saturated heterocyclic ring optionally substituted with a Cl-C4 alkyl group containing one or two O and/or S (O) p atoms in the ring; each R4 is independently selected from the group consisting of C1-C4 alkyl and Ci-C4 alkoxy; R5 is H, C1-C6 alkyl optionally substituted with R13, Cl-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6 alkynyl, C3-C6 haloalkynyl, Cl-C6 alkoxy, Cl-C6 haloalkoxy, C3-C6 alkynyloxy, C3-C6 haloalkenyloxy, C4-C6 cycloalkylalkoxy, C2-C6-cyanoalkoxy, phenylmethoxy, C2-C6 alkylcarbonyl, C3-C6 cycloalkylcarbonyl, phenylmethoxycarbonyl, formyl, C2-C6 haloalkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 haloalkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, hydroxy, phenylorbenzoyl(R15)(R16)P(O), each optionally substituted with one, two or three R17 substituents, naphthalenyl or a 5-or 6-membered unsaturated heterocyclic ring optionally substituted with one or two R17 substituents; R6 is G, H, C1-C6 alkyl, C1-C6 haloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, R14S (o) p, (R15) (Rl6) P (o) phenyl optionally substituted with one, two or three R17 substituents, naphthalenyl or a 5-or 6-membered unsaturated heterocyclic ring optionally substituted with one or two R17 substituents; or R5 and R6 with the nitrogen atom to which they are attached are taken together to form a: (1) 5-or 6-membered unsaturated heterocyclic ring optionally containing an additional heteroatom selected from N, O and S in the ring and optionally

containing one or two ring members C (=O), the ring optionally substituted with one or two R18 substituents; (2) 5-, 6-or 7-membered saturated heterocyclic ring optionally containing an additional heteroatom selected from N, O and S (O) p in the ring and optionally containing one or two ring members C (=O), the ring optionally substituted with one or two R18 substituents; or (3) 9-, 10-or 11-membered fused bicyclic ring system optionally containing an additional heteroatom selected from N, O and S (O) p in the ring and optionally containing one or two ring members C (=O), the ring optionally substituted with one or two R18 substituents; R7 is H, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C2-C4 alkylcarbonyl, C2-C4 alkoxycarbonyl, C2-C4 alkylaminocarbonyl or C3-C8 dialkylaminocarbonyl; each R8 is independently selected from the group H, C1-C4 alkyl and C3-C6 cycloalkyl; each R9 is independently selected from the group C1-C4 alkyl and C1-C4 haloalkyl; each R10 is independently selected from the group consisting of halogen, C1-C4 alkoxy, C1-C4 haloalkoxy, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, hydroxy, cyano, nitro, thiocyanato and R9S (O) p; each R11 is independently selected from the group C1-C4 alkyl and C1-C4 haloalkyl; each R12 is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl and Cl-C4 alkylsulfonyl; each R13 is independently selected from the group consisting of halogen, hydroxy, cyano, nitro, C3-C6 cycloalkyl, Ci-C4 alkoxy, C1-C4 haloalkoxy, phenylmethoxy, C2-C6 alkylcarbonyl, C2-C6 haloalkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 haloalkoxycarbonyl, C1-C4 alkylthio, C1-C4 alkylsulfinyl, Ci-C4 alkylsulfonyl, Ci-C4 haloalkylsulfonyl, aminocarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, R9S (O) p and phenyl optionally substituted with one, two or three R17 substituents; each R14 is independently selected from the group consisting of Ci-C4 alkyl, C1-C4 haloalkyl and phenyl optionally substituted with one, two or three R17 substituents; each R15 and each R16 are independently selected from the group consisting of Ci-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; each R17 is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, Ci-C4 haloalkoxy, Ci-C4 alkylthio, Cl-C4 alkylsulfinyl and C1-C4 alkylsulfonyl; each R18 is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C 1-C4 haloalkoxy,

R14S (O) p, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl and phenyl, phenylmethyl or pyridinyl each optionally substituted with one, two or three R17 substituents; m is 0,1 or 2; and each p is independently selected from 0,1 and 2.

In the above recitations, the term"alkyl", used either alone or in compound words such as"haloalkyl"includes straight-chain or branched alkyl, such as, methyl, ethyl, n-propyl, i-propyl, or the different butyl, pentyl or hexyl isomers."Alkenyl"includes straight-chain or branched alkenes such as ethenyl, 1-propenyl, 2-propenyl, and the different butenyl, pentenyl or hexenyl isomers."Alkenyl"also includes polyenes such as 1,2-propadienyl and 2,4-hexadienyl."Alkynyl"includes straight-chain or branched alkynes such as ethynyl, 1-propynyl, 2-propynyl and the different butynyl, pentynyl or hexynyl isomers."Alkynyl" can also include moieties comprised of multiple triple bonds such as 2,5-hexadiynyl. <BR> <BR> <P>"Alkylene"denotes a straight-chain or branched alkanediyl. Examples of"alkylene"include CH2, CH2CH2, CH (CH3), CH2CH2CH2, CH2CH (CH3) and the different butylene isomers.

"Alkoxy"includes, for example, methoxy, ethoxy, n-propyloxy, isopropyloxy and the different butoxy, pentoxy or hexyloxy isomers."Alkynyloxy"includes straight-chain or branched alkynyloxy moieties. Examples of"alkynyloxy"include HC=CCH20, CH3C=CCH20 and CH3C-CCH2CH2O."Cyanoalkoxy"denotes cyano substitution on alkoxy. Examples of"cyanoalkoxy"include NCCH20 and NCCH2CH2O.

"Alkylamino"denotes an amino group substituted with one alkyl group. Examples of "alkylamino"include CH3NH, CH3CH2NH, CH3CH2CH2NH, (CH3) 2CHNH and the different butylamino isomers. "Dialkylamino", and the like, are defined analogously to the above examples. Examples of"dialkylamino"include (CH3) 2N and (CH3) (CH3CH2) N.

"Dialkylaminocarbonyl"denotes dialkylamino substitution on carbonyl. Examples of "dialkylaminocarbonyl"include (CH3) 2NC (=O), (CH3CH2) 2NC (=O) and (CH3) (CH2CH2) NC (=O)."Alkylaminocarbonyl","aminocarbonyl"and the like, are defined analogously to the above examples."Phenylmethoxycarbonyl"denotes phenylmethoxy substitution on carbonyl [i. e., C6H5CH2OC (=O)]."Phenylcarbonyl"is defined analogously to the above examples.

"Cycloalkyl"includes, for example, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl."Cycloalkylalkoxy"denotes cycloalkyl substitution on alkoxy. Examples of <BR> <BR> "cycloalkylalkoxy"include cyclopropyl-CH20 and cyclohexyl-CH20."Cycloalkylcarbonyl" denotes cycloalkyl substitution on carbonyl. Examples of"cycloalkylcarbonyl"include cyclopropyl-C (=O) and cyclohexyl-C (=O).

Examples of G-1 heterocycles include optionally substituted 4-pyrimidinyl; 5,6,7,8- tetrahydro-4-quinazolinyl; 4-quinazolinyl; thieno [3,2-d] pyrimidin-4-yl; and thieno [2,3- d] pyrimidin-4-yl. Examples of G-2 heterocycles include optionally substituted 5-

isothiazolyl; 1,2,4-thiadiazol-5-yl; 5-isoxazolyl; 1H-pyrazol-5-yl; 1,2,4-oxadiazol-5-yl; and 1H-1,2,4-triazol-5-yl.

The term"unsaturated carbocyclic ring"includes fully aromatic carbocycles (where aromatic indicates that the Huckel rule is satisfied). The term"saturated carbocyclic ring" denotes fully saturated carbocycles. The term"unsaturated heterocyclic ring"includes fully aromatic heterocycles (where aromatic indicates that the Huckel rule is satisfied). The term "saturated heterocyclic ring"denotes fully saturated heterocycles.

Examples of R5 and/or R6 as a"5-or 6-membered unsaturated heterocyclic ring" include optionally substituted 2-pyridinyl, 3-pyridinyl, 4-pyridinyl and 2-thienyl.

An example of"R5 and R6 with the nitrogen atom at which they are attached taken together to for a 5-or 6-membered unsaturated heterocyclic ring optionally containing an additional heteroatom selected from N, O and S in the ring and optionally containing one or two ring members C (=O)" includes optionally substituted 2,5-dihydro-2,5-dioxo-lH- pyrrol-1-yl.

Examples of"R5 and R6 with the nitrogen atom at which they are attached taken together to for a 5-, 6-or 7-membered saturated heterocyclic ring (s) optionally containing an additional heteroatom selected from N, O and S (O) p in the ring and optionally containing one or two ring members C (=O)" include optionally substituted 1-piperidinyl, 4-morpholinyl, 1-piperazinyl and 2,5-dioxo-1-pyrrolidinyl.

Examples of"R5 and R6 with the nitrogen atom at which they are attached taken together to for a 9-, 10-or 11-membered fused bicyclic ring system optionally containing an additional heteroatom selected from N, O and S (O) p in the ring and optionally containing one or two ring members C (=O)" include optionally substituted 1,3-dihydro-1,3-dioxo-2H- isoindol-2-yl and octahydro-1,3-dioxo-2H-isoindol-2-yl.

The term"halogen", either alone or in compound words such as"haloalkyl", includes fluorine, chlorine, bromine or iodine. Further, when used in compound words such as "haloalkyl", said alkyl may be partially or fully substituted with halogen atoms which may be the same or different. Examples of"haloalkyl"include F3C, C1CH2, CF3CH2 and CF3CC12.

The terms"haloalkenyl","haloalkynyl","haloalkoxy","halocycloalky l","haloalkylcarbonyl" "haloalkoxycarbonyl"and the like, are defined analogously to the term"haloalkyl".

Examples of"haloalkenyl"include (C1) 2C=CHCH2 and CF3CH=CHCH2. Examples of <BR> <BR> <BR> "haloalkynyl"include HC_CCHC1, CF3C-C, CC13C-C and FCH2C-CCH2. Examples of "haloalkoxy"include CF30, CC13CH20, HCF2CH2CH20 and CF3CH20. Examples of "halocycloalkyl"include 2-chlorocyclopropyl and 2-fluorocyclohexyl. Examples of "haloalkylcarbonyl"include CF3C (=O), CC13CH2C (=O) and HCF2CH2CH2C (=O).

Examples of"haloalkoxycarbonyl"include CF30C (=O), CCl3CH20C (=O) and HCF2CH2CH20C (=O)."Haloalkenyloxy"denotes haloalkenyl substitution on alkoxy.

Examples of"haloalkenyloxy"include CF2=CF (CH2) 20 and CF2=CFCH20.

"Alkylthio"includes branched or straight-chain alkylthio moieties such as methylthio, ethylthio, and the different propylthio and butylthio isomers."Alkylsulfinyl"includes both enantiomers of an alkylsulfinyl group. Examples of"alkylsulfinyl"include CH3S (O), CH3CH2S (O), CH3CH2CH2S (O), (CH3) 2CHS (O) and the different butylsulfinyl isomers.

Examples of"alkylsulfonyl"include CH3S (0) 2, CH3CH2S (0) 2, CH3CH2CH2S (0) 2, (CH3) 2CHS (0) 2 and the different butylsulfonyl isomers.

The total number of carbon atoms in a substituent group is indicated by the"Ci-Cj" prefix where i and j are numbers from 1 to 8. For example, C2 alkylcarbonyl designates C (O) CH3 and C4 alkylcarbonyl designates C (O) CH2CH2CH3 and C (O) CH (CH3) 2.

Examples of"alkoxycarbonyl"include CH30C (=O), CH3CH20C (=O), CH3CH2CH20C (=O), (CH3) 2CHOC (=O) and the different butoxy-, pentoxycarbonyl, etc. isomers.

When a group contains a substituent which can be hydrogen, for example R2 or R7, then, when this substituent is taken as hydrogen, it is recognized that this is equivalent to said group being unsubstituted. When a group is optionally substituted with a substituent, for example with R17, then, when the group is not substituted with that substituent, it is recognized that this is equivalent to said group having a hydrogen substituent.

Compounds of this invention can exist as one or more stereoisomers. The various stereoisomers include enantiomers, diastereomers, atropisomers and geometric isomers (e. g., cis and trans cyclohexane isomers). For 1,4-disubstituted cyclohexanes, the cis isomer is preferred. One skilled in the art will appreciate that one stereoisomer may be more active and/or may exhibit beneficial effects when enriched relative to the other stereoisomer (s) or when separated from the other stereoisomer (s). Additionally, the skilled artisan knows how to separate, enrich, and/or to selectively prepare said stereoisomers. Accordingly, the present invention comprises compounds selected from Formula I and agriculturally suitable salts thereof. The compounds of the invention may be present as a mixture of stereoisomers, individual stereoisomers, or as an optically active form.

The salts of the compounds of the invention include acid-addition salts with inorganic or organic acids such as hydrobromic, hydrochloric, nitric, phosphoric, sulfuric, acetic, butyric, fumaric, lactic, maleic, malonic, oxalic, propionic, salicylic, tartaric, 4-toluenesulfonic or valeric acids. The salts of the compounds of the invention also include quaternary salts formed with alkyl halides (e. g., iodomethane, iodoethane or 1-chlorododecane). The salts of the compounds of the invention also include those formed with organic bases (e. g., pyridine, ammonia or triethylamine) or inorganic bases (e. g., hydrides, hydroxides or carbonates of sodium, potassium, lithium, calcium, magnesium or barium) when the compound contains an acidic group such as a carboxylic acid or phenol.

Preferred compounds for reasons of better activity and/or ease of synthesis are:

Preferred 1. Compounds of Formula I above, and agriculturally suitable salts thereof, wherein G-1;Gis Y is a direct bond; X is NR7; R1 is H or C1-C4 alkyl; R2 is C1-C4 alkyl, CF3, C3-C6 cycloalkyl, R1°CH2CH2-, (R1°) 2CHCH2-, R1°CH2CH (R10)-, CH3C (R1°) 2-, or C1 alkyl optionally substituted with C1-C4 alkoxy; R3 is C1-C4 alkyl, CF3, C1 alkyl optionally substituted with C1-C4 alkoxy, C2-C4 alkenyl, C2-C4 alkynyl, CI-C4 alkoxy, C1-C4 haloalkoxy, halogen, hydroxy, cyano, nitro, thiocyanato or R11S(O)p; and m is 0.

Preferred 2. Compounds of Preferred 1 above, and agriculturally suitable salts thereof, wherein R5 is H, C1-C6 alkyl optionally substituted with R13, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6 alkynyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C3-C6 alkynyloxy, C3-C6 haloalkenyloxy, C4-C6 cycloalkylalkoxy, C2-C6-cyanoalkoxy, phenylmethoxy, C2-C6 alkylcarbonyl, C3-C6 cycloalkylcarbonyl, phenylmethoxycarbonyl, formyl, C2-C6 haloalkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 haloalkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-C8 dialkylaminocarbonyl, hydroxy, R14S (O) p, or (R15) (Rl6) p (o); R6 is G, H, C1-C6 alkyl, C1-C6 haloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, R14S (O) p, (R15)(R16)P(O), phenyl optionally substituted with one, two or three R17 substituents, naphthalenyl or a 5- or 6-membered unsaturated heterocyclic ring optionally substituted with one or two R17 substituents; or R5 and R6 with the nitrogen atom to which they are attached are taken together to form a 1-piperazinyl; 2,5-dihydro- or 1,3-dihydro-1, 3-dioxo-2H-isoindol-2-yl; ring each optionally substituted with R18.

Preferred 3. Compounds of Preferred 2 above, and agriculturally suitable salts thereof, wherein R5 is H, C1-C6 alkyl optionally substituted with R13, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6 alkynyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C3-C6 alkynyloxy, C3-C6 haloalkenyloxy,

C4-C6 cycloalkylalkoxy, C2-C6-cyanoalkoxy, phenylmethoxy, C2-C6 alkylcarbonyl, C3-C6 cycloalkylcarbonyl, phenylmethoxycarbonyl, formyl, C2-C6 haloalkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 haloalkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, hydroxy, R14S (O) p, or (R15) (Rl6)pPp ; R6 is G, H, Cl-C6 alkyl, C1-C6 haloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, phenyl optionally substituted with one, two or three R17 substituents, or pyridinyl optionally substituted with one or two R17 substituents; or R5 and R6 with the nitrogen atom to which they are attached are taken together to form a 1-piperazinyl; 2,5-dihydro- or 1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl; ring each optionally substituted with R18.

Preferred 4. Compounds of Preferred 2 above, and agriculturally suitable salts thereof, wherein R5 is H, C1-C6 alkyl optionally substituted with R13, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6 alkynyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C3-C6 alkynyloxy, C3-C6 haloalkenyloxy, C4-C6 cycloalkylalkoxy, C2-C6-cyanoalkoxy, phenylmethoxy, C2-C6 alkylcarbonyl, C3-C6 cycloalkylcarbonyl, phenylmethoxycarbonyl, formyl, C2-C6 haloalkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 haloalkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-C8 dialkylaminocarbonyl, hydroxy, R14S (O) P, or (R15) (Rl6)pPp ; R6 is H, C1-C6 alkyl, C1-C6 haloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, phenyl optionally substituted with one, two or three R17 substituents, or pyridinyl optionally substituted with one or two R17 substituents; or R5 and R6 with the nitrogen atom to which they are attached are taken together to form a 1-piperazinyl; 2,5-dihydro- or ; ring each optionally substituted with R18.

Preferred 5. Compounds of Formula I above, and agriculturally suitable salts thereof, wherein G is G-2; Y is a direct bond; X is NR7;

Z1 is S; R2 is C1-C4 alkyl, C1-C4 haloalkoxy, C3-C6 cycloalkyl or C1 alkyl optionally substituted with C1-C4 alkoxy; R3 is C1-C4 alkyl, CF3, C1 alkyl optionally substituted with C 1-C4 alkoxy, C2-C4 alkenyl, C2-C4 alkynyl, Ci-C4 alkoxy, C1-C4 haloalkoxy, halogen, hydroxy, cyano, nitro, thiocyanato or R S (O) p ; and m is 0.

This invention also relates to arthropodicidal compositions comprising arthropodicidally effective amounts of the compounds of the invention and at least one of a surfactant, a solid diluent or a liquid diluent. The preferred compositions of the present invention are those which comprise the above preferred compounds.

This invention also relates to a method for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of the compounds of the invention (e. g., as a composition described herein). The preferred methods of use are those involving the above preferred compounds.

This invention also relates to fungicidal compositions comprising fungicidally effective amounts of the compounds of the invention and at least one of a surfactant, a solid diluent or a liquid diluent. The preferred compositions of the present invention are those which comprise the above preferred compounds.

This invention also relates to a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed or seedling, a fungicidally effective amount of the compounds of the invention (e. g., as a composition described herein). The preferred methods of use are those involving the above preferred compounds.

DETAILS OF THE INVENTION The compounds of Formula I can be prepared by one or more of the following methods and variations as described in Schemes 1-17. The definitions of G, G-1, G-2, Y, X, Z, Z1, m, p and R1-R22 in the compounds of Formulae I and 1-23 below are as defined above (including the Summary of the Invention) or below (including the Schemes). Compounds of Formulae Ia-Ib are various subsets of the compounds of Formula I, and all substituents for Formulae Ia-Ib are as defined above for Formula I.

Compounds of Formula I can be prepared by reaction of a heterocycle of Formula 1 with a compound of Formula 2 in the presence of an acid acceptor or a base. Typical bases can be triethylamine, pyridine, sodium hydride or potassium carbonate. The reaction can be carried out in the presence of a solvent such as toluene, tetrahydrofuran, acetonitrile, N, N-dimethylformamide or isopropanol. The reaction can be conducted in the temperature range ofO °C to the reflux temperature of the solvent. Scheme 1 depicts this transformation.

Scheme 1 ? CR4- ! base R3 |__ p6 rN/'A/ base I Y N , O, S) 2 2 N-'1 R R 1 I

x=m1, o, s E = F, Cl, Br, I, S02Me, S02Ar, OS02Me, OS02CF3, OS02Ar (e. g., OS02 (4-CH3-Ph)) Alternatively, compounds of Formula I can be prepared by reaction of a heterocycle of Formula 3 with a compound of Formula 4 in the presence of a base. Typical bases can include sodium hydride, potassium tert-butoxide or potassium carbonate. Typical solvents for the reaction include ether, tetrahydrofuran, acetonitrile or N, N-dimethylformamide. The reaction can be conducted in the temperature range ofO °C to the reflux temperature of the particular solvent. Scheme 2 depicts this transformation.

Scheme 2 XI 4) m R ton base L-Y \ I (X = NR, O, S) R2 RI RS 3 4

L L = F, Cl, Br, I, OS02Me,<BR> <BR> <BR> X =NR,0,SOSOCF3,OSOAr Alternatively, compounds of Formula I can be prepared by reaction of a heterocycle of Formula 3 (X = NR7) with a ketone of Formula 5 in the presence of a reducing agent. One skilled in the art will recognize said transformations as reductive aminations. A typical example of a reductive amination is described by Bagley et al. (J. Med. Chem. 1989,32, 663-671). The desired reductions can be performed with hydride agents such as sodium borohydride, sodium cyanoborohydride or sodium triacetoxyborohydride, or by catalytic hydrogenation (Hudlicky, M., Reductions in Organic Chemistry; Academic: New York, 1984). The reaction is typically conducted in methanol, ethanol, ether, tetrahydrofuran, dichloromethane, 1,2-dichloroethane or toluene in the presence of an additive such as hydrochloric or acetic acid. Scheme 3 depicts this transformation.

Scheme 3 Alternatively, compounds of Formula I can be prepared by reaction of a heterocycle of Formula 3 with an alcohol of Formula 2 (X = O) in the presence of a phosphine and an azodicarboxylate. One skilled in the art will recognize said reactions as Mitsunobu reactions (Hughes, D. L. Org. Prep. Proc. Int. 1996,28,127-164). Typical phosphines can include triphenylphosphine, tributylphosphine or trimethylphosphite. Typical azodicarboxylates can include diethyl azodicarboxylate (DEAD) or diisopropyl azodicarboxylate (DIAD). The reaction is typically conducted in ether, tetrahydrofuran, benzene or toluene. Scheme 4 depicts this transformation.

Scheme 4 Alternatively, compounds of Formula I can be prepared by reaction of an amine of Formula 6 with a compound of Formula 7 in the presence of a base. Typical bases can be triethylamine, pyridine, potassium carbonate or sodium bicarbonate. This reaction can be repeated with compounds of Formula 8 in the presence of another base to provide compounds of Formula I (R6 is other than H). Typical bases for the second reaction can include triethylamine, potassium carbonate, sodium hydride or potassium tert-butoxide.

Typical solvents for these reactions can be dichloromethane, ether, tetrahydrofuran, toluene, acetonitrile or N, N-dimethylformamide. The reaction can be conducted in the temperature range ofO °C to the reflux temperature of the solvent. When R6 is a phenyl group, the reaction can be carried out in the presence of either a palladium or a copper catalyst. Such reactions are well known to one skilled in the art. For example, conversion of aryl bromides into arylamines in the presence of a palladium catalyst is described by Buchwald et al.

(Angew. Chem. Int. Ed. Engl. 1995,34,1348-1350). Compounds of Formulae 7 and 8 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. Scheme 5 depicts this transformation.

Scheme 5

(R4hn R5-L R6-L I 7 X-Y ß NH2'I (R6is H)'I (R6isotherthan H) base base G-1 L = F, CL Br, I, OS02Me, OS02CF3, OS02Ar Alternatively, compounds of Formula I can be prepared by reductive amination of an amine of Formula 6 with a carbonyl compound of Formula 9. The reaction can be carried out in a manner analogous to Scheme 3 reactions to provide compounds of Formula I (R6 is H).

The carbonyl compounds of Formula 9 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. Scheme 6 depicts this transformation.

Scheme 6 R19 = H, Me, Et R20 = H, Me, Et, Ph Alternatively, compounds of Formula I can be prepared by reductive amination of a ketone of Formula 10 with an amine of Formula 11. The reaction can be carried out in a manner analogous to Scheme 3 reactions. The reaction also can be carried out in a stepwise manner. Such alternative procedures are well known to one skilled in the art. The amines of Formula 11 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. Scheme 7 depicts this transformation.

Scheme 7 amine Alternatively, compounds of Formula I can be prepared by displacement of a leaving group in a compound of Formula 12 by an amine of Formula 11 in the presence of a base.

The reaction can be carried out in a manner analogous to Scheme 5 reactions. Scheme 8 depicts this transformation.

Scheme 8 n? 4 (54) m 6 base i-Y L +. i--a I G-1 12 11 L = F, Cl, Br, I, OS02Me, amine amine OS02CF3,OS02Ar Alternatively, compounds of Formula I can be prepared by reaction of an alcohol of Formula 13 with an activated amide of Formula 14 under Mitsunobu conditions. Mitsunobu reactions were already described in detail in Scheme 4. The amides of Formula 14 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. Scheme 9 depicts this transformation.

Scheme 9

amide Alternatively, compounds of Formula la can be prepared by reaction of a heterocycle of Formula 1 with a diaminocyclohexane of Formula 15 in the presence of an acid acceptor or a base. The reaction is generally carried out with two or more equivalents of a heterocycle of Formula 1 in the presence of an excess amount of a base. Typical bases can be triethylamine, N, N-diisopropylethylamine, pyridine or potassium carbonate. The reaction can be carried out in the presence of a solvent such as toluene, tetrahydrofuran, acetonitrile, N, N-dimethylformamide or isopropanol. Typical reaction temperature can range from 0 °C to the reflux temperature of the particular solvent. The product can be derivatized further by reaction with compounds of Formula 7 in the presence of a base to provide compounds of Formula Ib (R5 is other than H). Typical bases for this can include sodium hydride, N, N-diisopropylethylamine, potassium tert-butoxide or potassium carbonate. Typical solvents can be ether, tetrahydrofuran, toluene, acetonitrile or N, N-dimethylformamide. The reaction can be conducted in the temperature range ofO °C to the reflux temperature of the solvent. The diaminocyclohexanes of Formula 15 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. An example of such preparation of diaminocyclohexanes is described by Johnston et al. (J. Med. Chem.

1977,20,279-290). Scheme 10 depicts this transformation.

Scheme 10 A )m G-1 base 1 + H2N NH2-. s G-1-H N H 15 Ia (R5is H) 5 (R4) G-1 7 g T/@ 1 base H > 5 R

Ib (R5 is other than H) Heterocycles of Formulae 1 and 3 can be prepared by a variety of literature methods or can be obtained from commercial sources. For example, pyrimidines of Formulae 1 and 3 can be prepared by procedures taught in U. S. Patent 4,977,264 and Foster et al. (Org. Synth.

1955,35,80-82), respectively. One skilled in the art will recognize that heterocycles of Formulae 1 and 3 can be interconverted by well-known chemistry. For example, heterocycles of Formula 1 (E = Cl, Br) can be converted into heterocycles of Formula 3 (X = O) by hydrolysis. Conversely, heterocycles of Formula 3 (X = NH) can be converted into heterocycles of Formula 1 (E = Cl, Br) by a Sandmeyer reaction (March, J. Advanced Organic Chemistry; 3rd ed.; John Wiley & Sons: New York, 1985; pp 647-648).

Compounds of Formula 2 can be prepared by reductive amination of a ketone of Formula 5 with an amine of Formula 16. The reaction can be carried out in a manner analogous to Scheme 3 reactions. Scheme 11 depicts this transformation.

Scheme 11 Alternatively, compounds of Formula 2 (X = NR7) can be prepared by reaction of a compound of Formula 4 with an amine of Formula 16 in the presence of a base. The reaction can be carried out in a manner analogous to Scheme 5 reactions. Compounds of Formula 2 (X = S) can be prepared by reaction of a compound of Formula 4 with a sulfur nucleophile of Formula 17 in the presence of a base. A typical sulfur nucleophile of Formula 17 can be thiourea, sodium hydrosulfide, sodium sulfide, potassium thioacetate, potassium thiocyanate, sodium thiophosphate or potassium O-ethyl xanthate. The utility of these reagents is well

known in literature. For example, the use of sodium thiophosphate is described by Bieniarz et al. (Tetrahedron Lett. 1993,34,939-942). The reaction of a compound of Formula 4 with sulfur nucleophile of Formula 17 may subsequently require a hydrolysis step in preparing compounds of Formula 2 (X = S). Scheme 12 depicts this transformation.

Scheme 12 H2NR7 16 4 + base 2 (X = NR7, S) or H2NC (S) NH2, NaSH, Na2S, AcSK KSCN, Na3P (S) 03, KSC (S) OEt 17 Alternatively, compounds of Formula 2 can be prepared from ketones of Formula 5 by a sequence of homologation reactions that are well known to one skilled in the art. For example, a ketone of Formula 5 is first converted into unsaturated ester of Formula 19 with a phosphonate of Formula 18 under Horner-Emmons olefination conditions (March, J.

Advanced Organic Chemistry; 3rd Ed.; John Wiley & Sons New York, (1985); p 848).

Compounds of Formula 19 then can be converted into compounds of Formula 2 (X-Y = OCH2CHR21) via catalytic hydrogenation followed by reduction. Phosphonates of Formula 18 can be obtained from commercial sources. Scheme 13 depicts this transformation.

Scheme 13 O4hn 22 R21 R6 5 + (EtO) 2P'C02R base/ N R21 R2202C \--/\5 R 18 19 R21 = H, Me R22 = Me, Et (i) catalytic hydrogenation 21 2 (X-Y = OCH2CHR) (ii) reduction Alternatively, compounds of Formula 2 can be prepared from aminocyclohexanols of Formula 20 by a sequence of reactions with compounds of Formulae 7 and 8 in the presence of a base. The reaction can be carried out in a manner analogous to Scheme 5 reactions.

Compounds of Formula 2 can be also prepared from cyclohexanediols of Formula 21 by Mitsunobu reaction with activated amide of Formula 14 in the presence of a phosphine and an azodicarboxylate. The reaction can be carried out in a manner analogous to Scheme 9 reactions. Compounds of Formulae 20 and 21 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. Scheme 14 depicts this transformation.

Scheme 14 4 4 2 (i) RL Mitsunobu (R4hn I'7 reaction HO--C 2 (X-Y = O) (fut) Ru-L R6 \--/ 20 8 14 21

amide L = F, Cl, Br, I, OS02Me, amie OS02CF3, OS02Ar Compounds of Formula 4 can be prepared from alcohols of Formula 2 (X = O) by a variety of literature methods. Such conversions of alcohols are well known to one skilled in the art (Carey, F. A.; Sundberg, R. J. Advanced Organic Chemistry; 2nd ed.; Plenum: New York, 1983; Part B, pp 95-101).

Compounds of Formula 5 can be prepared by oxidation of alcohols of Formula 2 (X-Y = O). One skilled in the art will recognize that ketones of Formula 5 and alcohols of Formula 2 (X-Y = O) can be interconverted by a variety of reduction and oxidation methods (March, J. Advanced Organic Chemistry; 3rd ed.; John Wiley & Sons: New York, 1985; pp 809-814,1057-1060).

Compounds of Formula 6 can be prepared by reductive amination of compounds of Formula 10 with ammonia in the presence of a reducing agent. The reaction can be carried out in a manner analogous to Scheme 7 reactions.

Alternatively, compounds of Formula 6 can be prepared by reaction of one or less equivalent of a heterocycle of Formula 1 with diaminocyclohexane of Formula 15 with or without a base. The reaction can be carried out in a manner analogous to Scheme 10 reactions. Scheme 15 depicts this transformation.

Scheme 15 (RV base 1 + H2N t N H2 or 6 (X-Y = NH) ou neat 15 Compounds of Formula 10 can be prepared by oxidation of alcohols of Formula 13.

One skilled in the art will recognize that ketones of Formula 10 and alcohols of Formula 13 can be interconverted by a variety of reduction and oxidation methods (March, J. Advanced Organic Chemistry; 3rd ed.; John Wiley & Sons: New York, 1985; pp 809-814,1057-1060).

Compounds of Formula 12 can be prepared from alcohols of Formula 13 by a variety of literature methods. Such conversions of alcohols are well known to one skilled in the art (Carey, F. A.; Sundberg, R. J. Advanced Organic Chemistry; 2nd ed.; Plenum: New York, 1983; Part B, pp 95-101).

Compounds of Formula 13 can be prepared by reaction of a heterocycle of Formula 1 with a compound of Formula 22 in the presence of a base. The reaction can be carried out in a manner analogous to Scheme 1 reactions. Scheme 16 depicts this transformation.

Scheme 16 (R4) m base 1 + HX-Y OH , O, S) 22

X = NR7, 0, S Compounds of Formula 22 can be obtained from commercial sources or prepared by conventional methods well known to one skilled in the art. For example, compounds of Formula 22 (X-Y = OCH2CHR21) can be prepared from cyclohexanediols of Formula 21 by oxidation followed by a sequence of reactions described in detail in Scheme 13. Scheme 17 depicts this transformation.

Scheme 17 (R4) m (R4) m oxidation Scheme 13 HO--6-OH-0-6-OH 22 (X-Y = OCH2CHR21) 21 23 15 20 Compounds of Formula I (G = G-2) can be prepared in a manner exactly analogous to reactions described in Schemes 1-17 for Formula I (G = G-1) compounds.

It is recognized that some reagents and reaction conditions described above for preparing compounds of Formula I may not be compatible with certain functionalities present in the intermediates. In these instances, the incorporation of protection and deprotection sequences or functional group interconversions into the synthesis will aid in obtaining the desired products. The use and choice of the protecting groups will be apparent to one skilled in chemical synthesis (see, for example, Greene, T. W. Protective Groups in Organic Synthesis; John Wiley & Sons: New York, 1981). One skilled in the art will recognize that, in some cases, after the introduction of a given reagent as it is depicted in any individual scheme, it can be necessary to perform additional routine synthetic steps not described in

detail to complete the synthesis of compounds of Formula I. One skilled in the art will also recognize that it can be necessary to perform a combination of the steps illustrated in the above schemes in an order other than that implied by the particular sequence presented to prepare the compounds of Formula I.

One skilled in the art will also recognize that compounds of Formula I and the intermediates described herein can be subjected to various electrophilic, nucleophilic, radical, organometallic, oxidation, and reduction reactions to add substituents or modify existing substituents.

Without further elaboration, it is believed that one skilled in the art using the preceding description can utilize the present invention to its fullest extent. The following Examples are, therefore, to be construed as merely illustrative, and not limiting of the disclosure in any way whatsoever. The title compound in each example is indicated by the abbreviation"Ex." followed by a number showing in which example the compound is prepared. Percentages are by weight except for chromatographic solvent mixtures or where otherwise indicated. Parts and percentages for chromatographic solvent mixtures are by volume unless otherwise indicated. 1H NMR spectra are reported in ppm downfield from tetramethylsilane; <BR> <BR> <BR> s = singlet, d = doublet, t = triplet, q = quartet, m = multiplet, dd = doublet of doublets, ddd = doublet of doublet of doublets, tt = triplet of triplets, br s = broad singlet, br d = broad doublet.

The following examples illustrate the invention: EXAMPLE 1 cis-N, N-Bis (5-chloro-6-ethyl-4-pyrimidinyl)-1, 4-cyclohexanediamine To a magnetically-stirred solution of 0.50 g (4.38 mmol) of 1,4-cyclohexanediamine (ca. cis/trans = 80/20) in 30 mL of acetonitrile were sequentially added 1.8 mL (13.14 mmol) of triethylamine and a solution of 1.63 g (9.20 mmol) of 4,5-dichloro-6-ethylpyrimidine in 10 mL of acetonitrile dropwise under nitrogen. The resultant clear solution was heated at reflux for 72 h. The mixture was cooled and diluted with ethyl acetate and water. The layers were separated and the aqueous layer was extracted with ethyl acetate (2x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 10%, 40%, then 60% ethyl acetate/hexane to afford 1.10 g (64%) of the title compound (Ex. 1) as a white solid, melting at 119-121 °C. 1H NMR (CDC13): 8 8.43 (s, 2H), 5.43 (d, 2H), 4.22 (m, 2H), 2.80 (q, 4H), 1.96 (m, 4H), 1.76 (m, 4H), 1.27 (t, 6H).

EXAMPLE 2 (a) cis-N- (5-Chloro-6-ethvl-4-p. vrimidinyl)-N-(5-chloro-6-ethvl-4-pvrimidinyl)-N-methyl- 1,4-cyclohexanediamine, (b) cis-NS-bis (5-chloro-6-ethvl-4-perimidinel)-NS-dimethYl- 1, 4-cyclohexanediamine and (c) cis-N-(5-chloro-6-ethyl-4-pyrimidinyl)-N'-r5-chloro-6- (1- methylethylLpyrimidinyll-N, N'-dimethyl-1, 4-cyclohexanediamine To a magnetically-stirred suspension of 0.28 g (7.06 mmol) of sodium hydride (60 wt% dispersion in mineral oil) in 20 mL of N, N dimethylformamide was added a solution of 0.93 g (2.35 mmol) of cis-N, N'-bis (5-chloro-6-ethyl-4-pyrimidinyl)-1,4-cyclohexanediamine in 10 mL of N, N-dimethylformamide dropwise under nitrogen. The resultant mixture was heated and stirred at 85-90 °C for 40 min and a solution of 0.44 mL (7.06 mmol) of iodomethane in 10 mL of N, N-dimethylformamide was added dropwise. The resultant clear yellow solution was stirred at the same temperature overnight. The mixture was cooled and poured onto a diethyl ether-water solution. The layers were separated and the aqueous layer was extracted with diethyl ether (2x). The combined organic layers were washed with water and brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 20%, 30%, 40%, 50%, then 100% ethyl acetate/hexane to afford 0.07 g (6%) of cis-N-(5- <BR> <BR> <BR> chloro-6-ethyl-4-pyrimidinyl)-N'- [5-chloro-6- (l-methylethyl)-4-pyrimidinyl]-N, N'-dimethyl- 1,4-cyclohexanediamine (Ex. 2c) as a white solid, melting at 95-97 °C, 1H NMR (CDC13): <BR> <BR> <BR> 6 8.57 (s, 1H), 8.52 (s, 1H), 4.07 (m, 2H), 3.54 (m, 1H), 2.96 (s, 3H), 2.94 (s, 3H), 2.88 (q, 2H), 2.06 (m, 4H), 1.61 (m, 4H), 1.30 (t, 3H), 1.26 (d, 6H), 0.21 g (21%) of cis-N,N'-bis (5- chloro-6-ethyl-4-pyrimidinyl)-N, N'-dimethyl-1, 4-cyclohexanediamine (Ex. 2b) as a white solid, melting at 86-87 °C, IH NMR (CDC13): 6 8.53 (s, 2H), 4.07 (m, 2H), 2.96 (s, 6H), 2.89 (q, 4H), 2.05 (m, 4H), 1.61 (m, 4H), 1.30 (t, 6H), and 0.16 g (16%) of cis-N- (5-chloro- 6-ethyl-4-pyrimidinyl)-N-(5-chloro-6-ethyl-4-pyrimidinyl)-N- methyl-1, 4- cyclohexanediamine (Ex. 2a) as a white solid, melting at 68-70 °C, 1H NMR (CDC13): 5 8.45 (s, 1H), 8.43 (s, 1H), 5.58 (br d, 1H), 4.33 (m, 1H), 4.18 (m, 1H), 3.03 (s, 3H), 2.86 (q, 2H), 2.81 (q, 2H), 2.10 (m, 2H), 1.81 (m, 6H), 1.29 (t, 3H), 1.28 (t, 3H).

EXAMPLE 3 cis-N. (5-chloro-6-ethvl-4-pyrimidinyl)-1, 4-cvclohexanediamine dihydrochloride To a magnetically-stirred solution of 0.72 g (1.82 mmol) of cis-NN-bis (5-chloro-6- ethyl-4-pyrimidinyl)-1,4-cyclohexanediamine in 20 mL of dichloromethane was added 5 mL of 1 M HC1 solution in methanol. The resultant mixture was stirred at room temperature overnight and concentrated at reduced pressure. The solid residue was washed with dichloromethane and diethyl ether, and dried to afford 0.51 g (60%) of the title compound (Ex. 3) as a white solid, melting at 239-242 °C, 1H NMR (DMSO-d6): 8 8.67 (s, 2H), 7.73 (br s, 2H), 4.27 (m, 2H), 2.82 (q, 4H), 1.95 (m, 4H), 1.71 (m, 4H), 1.22 (t, 6H).

EXAMPLE 4 cis-N-(5-Chloro-6-ethyl-4-pyrimidinyl)-N'-(4-quinazolinyl)-1 4-cyclohexanediamine To a magnetically-stirred solution of 0.50 g (4.38 mmol) of 1,4-cyclohexanediamine (ca. cis/trans = 80/20) in 30 mL of acetonitrile were sequentially added 1.8 mL (13.14 mmol) of triethylamine and a solution of 0.78 g (4.38 mmol) of 4,5-dichloro-6-ethylpyrimidine in 10 mL of acetonitrile dropwise under nitrogen. The clear solution was heated at reflux for 1 h. The resultant mixture was cooled to 40 °C and a slurry of 0.72 g (4. 38 mmol) of 4-chloroquinazoline in 10 mL of acetonitrile was added. The resultant mixture was heated at reflux overnight. The mixture was cooled and diluted with ethyl acetate and water. The layers were separated and the aqueous layer was saturated with sodium chloride and extracted with ethyl acetate (2x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The solid residue was purified by silica gel flash column chromatography eluting with ethyl acetate to afford 0.24 g (14%) of the title compound (Ex. 4) as a white solid, melting at 188-191 °C. 1H NMR (CDC13): 8 8.68 (s, 1H), 8.44 (s, 1H), 7.86 (d, 1H), 7.75 (m, 2H), 7.49 (ddd, 1H), 5.69 (br d, 1H), 5.46 (br d, 1H), 4.47 (m, 1H), 4.28 (m, 1H), 2.80 (q, 2H), 2.05 (m, 4H), 1.84 (m, 4H), 1.28 (t, 3H).

EXAMPLE 5 Step A: trans-4- [ 5-chloro-6-ethvl-4-pvrimidinvl) aminolcyclohexanol To a magnetically-stirred solution of 1.00 g (8.68 mmol) of trans-4-aminocyclohexanol in 40 mL of acetonitrile were sequentially added 1.8 mL (13.02 mmol) of triethylamine and a solution of 1.69 g (9.55 mmol) of 4,5-dichloro-6-ethylpyrimidine in 10 mL of acetonitrile dropwise under nitrogen. The pale yellow solution was heated at reflux overnight. The resultant clear orange mixture was cooled and diluted with ethyl acetate and water. The layers were separated and the aqueous layer was saturated with NaCl and extracted with ethyl acetate (2x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 50%, then 100% ethyl acetate/hexane to afford 1.87 g (84%) of trans-4- [ (5-chloro-6-ethyl-4-pyrimidinyl) amino] cyclohexanol as a <BR> <BR> <BR> white solid, melting at 138-139 °C, 1H NMR (CDC13): 6 8.41 (s, 1H), 5.16 (br d, 1H), 3.99 (m, 1H), 3.69 (m, 1H), 2.78 (q, 2H), 2.15 (m, 2H), 2.04 (m, 2H), 1.50 (m, 2H), 1.48 (d, 1H), 1.32 (m, 2H), 1.26 (t, 3H).

Step B: 4-r (5-chloro-6-ethyl-4-pyrimidinyl) amino] cyclohexanone To a magnetically-stirred solution of 2.00 g (7.82 mmol) of trans-4- [ (5-chloro-6-ethyl- 4-pyrimidinyl) amino] cyclohexanol in 60 mL of dichloromethane was added 2.02 g (9.38 mmol) of pyridinium chlorochromate in one portion. The resultant black mixture was stirred at room temperature overnight. The mixture was diluted with ethyl acetate and filtered through a short pad of silica gel. The black solid that remained behind was dissolved

in 1 N aqueous NaOH solution and extracted with ethyl acetate (3x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with ethyl acetate to afford 1.58 g (80%) of 4- [ (5-chloro-6-ethyl-4- pyrimidinyl) amino] cyclohexanone as a white solid, melting at 115-116 °C, IH NMR (CDC13): 5 8.45 (s, 1H), 5.29 (d, 1H), 4.49 (m, 1H), 2.80 (q, 2H), 2.63-2.34 (m, 6H), 1.81 (m, 2H), 1.27 (t, 3H).

Step C: (a) cis-N-(5-Chloro-6-ethyl-4-pyrimidinyl)-Nt-phenyl-ls4-cyclohe xanediamine and (b) trans-N-(5-chloro-6-ethyl-4-pyrimidinyl)-N'-phenyl-1, 4- cyclohexanediamine To a magnetically-stirred solution of 1.00 g (3.94 mmol) of 4- [ (5-chloro-6-ethyl-4- pyrimidinyl) amino] cyclohexanone in 50 mL of 1,2-dichloroethane were sequentially added 0.37 g (3.94 mmol) of aniline, 1.67 g (7.88 mmol) of sodium triacetoxyborohydride and 0.24 g (3.94 mmol) of glacial acetic acid under nitrogen. The resultant cloudy white mixture was stirred at room temperature overnight. The mixture was diluted with diethyl ether and washed with 1 N aqueous NaOH solution. The aqueous wash was extracted with diethyl ether (2x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 20%, then 50% ethyl acetate/hexane to afford 0.60 g (46%) of cis-N-(5-chloro-6-ethyl-4-pyrimidinyl)-N'-phenyl-1,4- <BR> <BR> <BR> cyclohexanediamine (Ex. 5a) as a white solid, melting at 88-93 °C, 1H NMR (CDC13): 6 8.42 (s, 1H), 7.18 (dd, 2H), 6.69 (t, 1H), 6.62 (d, 2H), 5.40 (br d, 1H), 4.19 (m, 1H), 3.71 (br s, 1H), 3.54 (m, 1H), 2.79 (q, 2H), 1.89 (m, 4H), 1.73 (m, 4H), 1.27 (t, 3H) and 0.57 g (44%) of trans-N-(5-chloro-6-ethyl-4-pyrimidinyl)-N-phenyl-1,(5-chlor o-6-ethyl-4-pyrimidinyl)-N-phenyl-1, 4-cyclohexanediamine (Ex. 5b) as a <BR> <BR> <BR> white solid, melting at 137-139 °C, 1H NMR (CDC13): 6 8.42 (s, 1H), 7.17 (dd, 2H), 6.68 (t, 1H), 6.60 (d, 2H), 5.21 (d, 1H), 4.03 (m, 1H), 3.51 (s, 1H), 3.31 (m, 1H), 2.79 (q, 2H), 2.21 (m, 4H), 1.37 (m, 4H), 1.26 (t, 3H).

EXAMPLE 6 cis-N'-(5-Chloro-6-ethyl-4-pyrimidinyl)-N-phenyl-N-2-propyny l-1,4-cyclohexanediamine To a magnetically-stirred solution of 0.40 g (1.21 mmol) of cis-N-(5-chloro-6-ethyl-4- pyrimidinyl)-N'-phenyl-1,4-cyclohexanediamine in 10 mL of toluene were sequentially added 0.31 mL (1.81 mmol) of N, N diisopropylethylamine and 0.13 mL (1.45 mmol) of 80 wt% propargyl bromide solution in toluene dropwise under nitrogen. The clear red solution was heated at reflux overnight. The resultant mixture was cooled and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 8%, then 100% acetone/dichloromethane to afford 0.32 g (72%) of the title compound (Ex. 6) as an orange viscous oil, 1H NMR (CDC13): 5 8.42 (s, 1H), 7.28 (m, 2H),

6.99 (m, 2H), 6.86 (t, 1H), 5.57 (d, 1H), 4.31 (m, 1H), 3.99 (d, 2H), 3.70 (m, 1H), 2.80 (q, 2H), 2.22 (t, 1H), 2.04 (m, 2H), 1.94-1.68 (m, 6H), 1.27 (t, 3H).

EXAMPLE 7 (a) cis-N'- (5-Chloro-6-ethyl-4-pvrimidinyl)-N*N-dimethyl-1. 4-cyclohexanediamine and (b) trans-N'- (5-chloro-6-ethyl-4-pyrimidinvl)-N, N-dimethyl-1, 4-cvclohexanediamine To a magnetically-stirred solution of 3.00 g (11.82 mmol) of 4- [ (5-chloro-6-ethyl-4- pyrimidinyl) amino] cyclohexanone in 120 mL of toluene were sequentially added 0.11 g (0.59 mmol) ofp-toluenesulfonic acid monohydrate and 5 mL of water containing 0.96 g (11.82 mmol) of dimethylamine hydrochloride. The clear mixture was stirred at reflux for 4 h with the water removed azeotropically through a Dean-Stark trap. The mixture was cooled to room temperature and to this were sequentially added 3.76 g (23.64 mmol) of sodium triacetoxyborohydride and 0.68 mL (11.82 mmol) of glacial acetic acid. The resultant cloudy white mixture was stirred at room temperature overnight. The mixture was quenched with 6 mL of 1 M aqueous NaHC03 solution and concentrated at reduced pressure.

The residue was purified by silica gel flash column chromatography eluting with 10%, 12%, then 15% methanol/dichloromethane to afford 0.58 g (17%) of cis-N- (5-chloro-6-ethyl-4- pyrimidinyl)-N, N-dimethyl-1,4-cyclohexanediamine (Ex. 7a) as a yellow solid, melting at <BR> <BR> <BR> 62-66 °C, 1H NMR (CDC13): 8 8.40 (s, 1H), 5.48 (d, 1H), 4.22 (m, 1H), 2.78 (q, 2H), 2.32 (s, 6H), 2.16 (m, 1H), 1.95-1.60 (m, 8H), 1.26 (t, 3H) and 0.87 g (26%) of trans-N'- (5- chloro-6-ethyl-4-pyrimidinyl)-N, N-dimethyl-1,4-cyclohexanediamine (Ex. 7b) as a yellow viscous oil, 1H NMR (CDC13): 5 8.40 (s, 1H), 5.19 (d, 1H), 3.94 (m, 1H), 2.78 (q, 2H), 2.38 (m, 1H), 2.36 (s, 6H), 2.21 (m, 2H), 2.01 (m, 2H), 1.47 (m, 2H), 1.28 (m, 2H), 1.26 (t, 3H).

EXAMPLE 8 cis-4-[(5-Chloro-6-ethyl-4-pyrimidinyl) aminol-NNnN-trimethylcyclohexanaminium[(5-Chloro-6-ethyl-4-p yrimidinyl) aminol-NNnN-trimethylcyclohexanaminium iodide To a magnetically-stirred solution of 0.30 g (1.06 mmol) of cis-N- (5-chloro-6-ethyl-4- pyrimidinyl)-N, N-dimethyl-1, 4-cyclohexanediamine in 10 mL of dichloromethane was added 0.72 mL (11.6 mmol) of iodomethane dropwise under nitrogen. The clear tan solution was stirred at room temperature overnight and concentrated at reduced pressure. The solid residue was oven-dried to afford 0.45 g (100%) of the title compound (Ex. 8) as a white solid, melting at 217-221 °C, 1H NMR (DMSO-d6): 6 8.38 (s, 1H), 6.44 (d, 1H), 4.21 (m, 1H), 3.35 (m, 1H), 3.03 (s, 3H), 2.72 (q, 2H), 2.13 (m, 2H), 1.98 (m, 2H), 1.78 (m, 2H), 1.67 (m, 2H), 1.18 (t, 3H).

EXAMPLE 9 Step A: cis-N-(5-chloro-6-ethyl-4-pyrimidinyl 4-cyclohexanediamine To a magnetically-stirred solution of 6.45 g (56.5 mmol) of 1,4-cyclohexanediamine (ca. cis/trans = 90/10) in 80 mL of acetonitrile was added a solution of 2.00 g (11.3 mmol) of 4,5-dichloro-6-ethylpyrimidine in 20 mL of acetonitrile dropwise under nitrogen. The resultant mixture was stirred at room temperature for 72 h. The cloudy white mixture was

concentrated to a volume of approximately 20 mL and diluted with diethyl ether and water.

The layers were saturated with NaCl and were separated, and the aqueous layer was extracted with diethyl ether (2x). The combined organic layers were washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated at reduced pressure. The oil residue was oven-dried to afford 2.94 g (100%) of cis-N- (5-chloro-6-ethyl-4-pyrimidinyl)-1,4- cyclohexanediamine as a tan solid, melting at 76-79 °C, 1H NMR (CDC13): 5 8.41 (s, 1H), 5.46 (d, 1H), 4.19 (m, 1H), 2.98 (m, 1H), 2.78 (q, 2H), 1.92-1.68 (m, 6H), 1.45 (m, 2H), 1.27 (m, 2H), 1.26 (t, 3H). Azeotropic distillation of the aqueous layer in toluene gave 3.11 g (61% recovery) of 1,4-cyclohexanediamine as an orange oil.

Step B: cis-N-(5-Chloro-6-ethyl-4-pyrimidinyl)-Nt-F5-methoxy-6-(meth oxYmethyl)-4- pvrimidinyll-1,4-cyclohexanediamine To a magnetically-stirred solution of 0.30 g (1.18 mmol) of cis-N- (5-chloro-6-ethyl-4- pyrimidinyl)-1,4-cyclohexanediamine in 10 mL of toluene were sequentially added 0.31 mL (1.77 mmol) of N, N-diisopropylethylamine and 0.24 g (1.30 mmol) of 4-chloro-5-methoxy-6- (methoxymethyl) pyrimidine under nitrogen. The clear solution was heated at reflux overnight. The resultant mixture was cooled and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 50%, 100% ethyl acetate/hexane, then 5% methanol/dichloromethane to afford 0.11 g (23%) of the title compound (Ex. 9) as a tan solid, which starts to melt at 104 °C, 1H NMR (CDC13): 5 8.42 (s, 1H), 8. 38 (s, 1H), 5.41 (d, 1H), 5.31 (d, 1H), 4.47 (s, 2H), 4.20 (m, 2H), 3.83 (s, 3H), 3.49 (s, 3H), 2.80 (q, 2H), 1.95 (m, 4H), 1.75 (m, 4H), 1.27 (t, 3H).

EXAMPLE 10 cis-2-r4-r(5-Chloro-6-ethyl-4-pyrimidinyl) aminolcyclohexyll-lH-isoindole-1, 3 (2H) dione To a magnetically-stirred solution of 0.60 g (2.36 mmol) of cis-N-(5-chloro-6-ethyl-4- pyrimidinyl)-1,4-cyclohexanediamine in 20 mL of tetrahydrofuran was added a solution of 0.35 g (2.36 mmol) of phthalic anhydride in 10 mL of tetrahydrofuran dropwise under nitrogen. The clear yellow solution was heated at reflux for 2 h. The resultant mixture was cooled and concentrated. The solid residue was dissolved in 5 mL of N, N dimethylformamide and approximately 1 g of polyphosphoric acid was added. The resultant mixture was heated at 80 °C for 2 h and poured onto a mixture of diethyl ether and 1 M aqueous NaHC03 solution. The layers were separated and the aqueous layer was extracted with diethyl ether (2x). The combined organic layers were washed with water and brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 40%, 70%, then 100% ethyl acetate/hexane to afford 0.20 g (22%) of the title compound (Ex. 10) as a white solid, melting at 157-160 °C, 1H NMR (CDC13): 5 8.43 (s, 1H), 7.84 (m, 2H), 7.72 (m, 2H), 5.88 (d, 1H), 4.47 (m, 1H), 4.25 (tt, 1H), 2.82 (q, 2H), 2.47 (m, 2H), 2.09 (m, 2H), 1.83-1.66 (m, 4H), 1.29 (t, 3H).

EXAMPLE 11 Step A: 4-r (5-chloro-6-ethyl-4-pyrimidinyl) aminolcyclohexanone O-methyloxime To a magnetically-stirred solution of 1.00 g (3.94 mmol) of 4- [ (5-chloro-6-ethyl-4- pyrimidinyl) amino] cyclohexanone in 10 mL of pyridine was added 0.40 g (4.73 mmol) of methoxyamine hydrochloride in one portion. The clear yellow mixture was stirred at room temperature overnight. The resultant mixture was diluted with dichloromethane and washed with water. The aqueous wash was extracted with dichloromethane (2x). The combined organic layers were washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 50% ethyl acetate/hexane to afford 0.99 g (89%) of 4- [ (5- chloro-6-ethyl-4-pyrimidinyl) amino] cyclohexanone O-methyloxime as a white solid, melting at 105-106 °C, 1H NMR (CDC13): 5 8.42 (s, 1H), 5.25 (d, 1H), 4.24 (m, 1H), 3.84 (s, 3H), 3.18 (m, 1H), 2.79 (q, 2H), 2.47 (m, 1H), 2.36-2.00 (m, 4H), 1.51 (m, 2H), 1.26 (t, 3H).

Step B: (a) cis-N-(5-Chloro-6-ethvl-4-pyrimidinyl)-N'-methoxy-1*4- cyclohexanediamine and (b) trans-N-(5-chloro-6-ethyl-4-pyrimidinyl)-N- methoxy-1,4-cyclohexanediamine To a cooled (0 °C), magnetically-stirred solution of 0.28 g (1.06 mmol) of 4- [ (5- chloro-6-ethyl-4-pyrimidinyl) amino] cyclohexanone O-methyloxime in 5 mL of ethanol were sequentially added dropwise 0.44 mL (3.53 mmol) of borane-pyridine complex and 4 mL of 10% aqueous HC1 solution. The clear mixture was allowed to warm to room temperature and stirred for 10 min. The resultant mixture was quenched with 1 M aqueous NaHC03 solution and diluted with ethyl acetate. The layers were separated and the aqueous layer was extracted with ethyl acetate (2x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 55%, 70%, then 100% ethyl acetate/hexane to afford 0.11 g (36%) of cis-N-(5-chloro-6-ethyl-4-pyrimidinyl)- N'-methoxy-1, 4-cyclohexanediamine (Ex. 1 la) as a clear oil, 1H NMR (CDC13): 5 8.41 (s, 1H), 5.47 (br s, 1H), 5.42 (br d, 1H), 4.18 (m, 1H), 3.58 (s, 3H), 3.07 (m, 1H), 2.78 (q, 2H), 1.87-1.55 (m, 8H), 1.26 (t, 3H) and 0.15 g (50%) oftrans-N-(5-chloro-6-ethyl-4- pyrimidinyl)-N'-methoxy-1,4-cyclohexanediamine (Ex. 1 lb) as a white solid, melting at 87- 88 °C, 1H NMR (CDC13): 8 8.41 (s, 1H), 5.43 (br s, 1H), 5.18 (br d, 1H), 3.98 (m, 1H), 3.55 (s, 3H), 2.90 (m, 1H), 2.78 (q, 2H), 2.18 (m, 2H), 2.00 (m, 2H), 1.31 (m, 4H), 1.26 (t, 3H).

EXAMPLE 12 cis-N-r4- [(5-Chloro-6-ethyl-4-vrimidinvl) aminolcyclohexvll-N-methoxyacetamide To a magnetically-stirred solution of 0.50 g (1.75 mmol) of cis-N-(5-chloro-6-ethyl-4- pyrimidinyl)-N'-methoxy-1,4-cyclohexanediamine in 20 mL of dichloromethane were sequentially added 0.17 mL (1.75 mmol) of acetic anhydride, 0.21 g (1.75 mmol) of 4- (dimethylamino) pyridine and 0.24 mL (1.75 mmol) of triethylamine under nitrogen. The

clear mixture was stirred at room temperature for 72 h. The resultant mixture was diluted with diethyl ether and water. The layers were separated and the aqueous layer was extracted with diethyl ether (2x). The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated at reduced pressure. The residue was purified by silica gel flash column chromatography eluting with 15%, 17.5%, then 20% acetone/hexane to afford 0.45 g (79%) of the title compound (Ex. 12) as a clear viscous oil, 1H NMR (CDC13): 8 8.42 (s, 1H), 5.61 (d, 1H), 4. 33 (m, 1H), 4.28 (m, 1H), 3.79 (s, 3H), 2.80 (q, 2H), 2.16 (s, 3H), 2.06 (m, 2H), 1.97-1.68 (m, 6H), 1.27 (t, 3H).

By the procedures described herein together with methods known in the art, the following compounds of Tables 1 to 26 can be prepared. The following abbreviations are used in the Tables which follow: t = tertiary, s = secondary, n = normal, i = iso, c = cyclo, Me = methyl, Et = ethyl, Pr = propyl, Bu = butyl, Pen = pentyl, t-Am = 1,1-dimethylpropyl, Hex = hexyl, Ph = phenyl, Bn = phenylmethyl, OMe = methoxy, OEt = ethoxy, CN = cyano, SMe = methylthio, Piper= Morph = Phth = Hphth = Key for Tables 1-26 Tables 1 to 3 Table 4 Tables 5 to 8 Tables 9 to 16 Tables 17 and 18 Table 19 Tables 20 Table 21 Table 22 Table 23 Tables 24 to 26 TABLE 1 COLUMN 312 =Q-1;R6=Me;R5=MeEtn-Pr1G 2 G = Q-1 ; R6 = Me ; R5 = i-Pr c-Pr n-Bu 3 G = Q-1 ; R6 = Me ; R5 = i-Bu t-Bu n-Hex =Q-1;R6=Me;R5=c-HexBnCH2CH=CH24G 5 G = Q-1 ; R6 = Me; R5 = CH2CCl= CH2 CH2C#CH CH2-c-Pr =Q-1;R6=Me;R5=CH2CNCH2CONH2CH2CONHMe6G 7 G = Q-1 ; R6 = Me; R5 = CH2CONMe2 CH20Me CH20Bn 8 G = Q-1 ; R6 = Me; R5 = CH2SMe CH2S (O) Me CH2S02Me 9 G = Q-1 ; R6 = Me; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 10 G = Q-1 ; R6 = Me ; R5 = OH OMe OEt =Q-1;R6=Me;11G OBnOCH2C#CHOCH2-c-Pr= 12 G = Q-1 ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 13 G = Q-1 ; R6 = Me; R5 = COMe COEt COCF3 14 G = Q-1 ; R6 = Me; R5 = CO-i-Pr CO-c-Pr COPh 15 G = Q-1 ; R6 = Me; R5 = CH2C02Me C02Me C02Et =Q-1;R6=Me;R5=CO2BnCONHMeSO2Ph16G =Q-1;R6=Ph;17G MeEtn-Pr= 18 G = Q-1 ; R6 = Ph ; R5 = i-Pr c-Pr n-Bu 19 G = Q-1 ; R6 = Ph ; R5 = i-Bu t-Bu n-Hex =Q-1;R6=Ph;20G c-PenBnCH2CH=CH2= 21 G = Q-1; R6 = Ph; R5 = CH2CCl= CH2 CH2C#CH CH2-c-Pr 22 G = Q-1 ; R6 = Ph; R5 = CH2CN CH2CONH2 CH2CONHMe 23 G = Q-1 ; R6 = Ph; R5 = CH2CONMe2 CH20Me CH20Bn =Q-1;R6=Ph;24G CH2SMeCH2S(O)MeCH2SO2Me= 25 G = Q-1 ; R6 = Ph; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 =Q-1;R6=Ph;26G OHOMeOEt= 27 G = Q-1 ; R6 = Ph; RS = OBn OCH2C=CH OCH2-c-Pr 28 G = Q-1 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 29 G = Q-1 ; R6 = Ph; R5 = COMe COEt COCF3 30 G = Q-1; R6 = Ph; R5 = CO-i-Pr CO-c-Pr COPh 31 G = Q-1; R6 = Ph; R5 = CH2CO2Me CO2Me CO2Et 32 G = Q-1; R6 = Ph; R5 = CO2Bn CONHMe SO2Ph 33 G = Q-2; R6 = Me; R5 = Me Et n-Pr 34 G = Q-2; R6 = Me; R5 = i-Pr c-Pr n-Bu 35 G = Q-2; R6 = Me; R5 = i-Bu t-Bu n-Hex 36 G = Q-2; R6 = Me; R5 = c-Hex Bn CH2CH=CH2 37 G = Q-2; R6 = Me; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 38 G = Q-2; R6 = Me; R5 = CH2CN CH2CONH2 CH2CONHMe 39 G = Q-2; R6 = Me; R5 = CH2CONMe2 CH20Me CH20Bn 40 G = Q-2; R6 = Me; R5 = CH2SMe CH2S (O) Me CH2SO2Me 41 G = Q-2; R6 = Me; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 42 G = Q-2; R6 = Me; R5 = OH OMe OEt 43 G = Q-2; R6 =OBnOCH2C=CHOCH2-c-Pr 44 G = Q-2; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 45 G = Q-2; R6 = Me ; R5 = COMe COEt COCF3 46 G = Q-2; R6 = Me; R5 = CO-i-Pr CO-c-Pr COPh 47 G = Q-2; R6 = Me; R5 = CH2C02Me C02Me C02Et 48 G = Q-2; R6 =C02BnCONHMeS02Ph 49 G = Q-2; R6 = Ph; R5 = Me Et n-Pr 50 G = Q-2; R6 = Ph; R5 = i-Pr c-Pr n-Bu 51 G = Q-2; R6 = Ph; R5 = i-Bu t-Bu n-Hex 52 G = Q-2; R6 = Ph; R5 = c-Pen Bn CH2CH=CH2 =Q-2;53G Ph;R5=CH2CCl=CH2CH2C#CHCH2-c-Pr= =Q-2;54G Ph;R5=CH2CNCH2CONH2CH2CONHMe= 55 G = Q-2; R6 = Ph; R5 = CH2CONMe2 CH20Me CH20Bn 56 G = Q-2; R6 = Ph; R5 = CH2SMe CH2S (O) Me CH2SO2Me 57 G = Q-2; R6 = Ph; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 58 G = Q-2; R6 = Ph; R5 = OH OMe OEt 59 G = Q-2; R6 = Ph; R5 = OBn OCH2C=CH OCH2-c-Pr 60 G = Q-2 ; R6 = Ph ; RS = OCH2CN O (CH2) 2CF=CF2 CHO 61 G = Q-2; R5=COMeCOEtCOCF3 62 G = Q-2; R6 = Ph; R5 = CO-i-Pr CO-c-Pr COPh 63 G = Q-2; R6 = Ph; R5 = CH2CO2Me CO2Me CO2Et 64 G = Q-2; R6 = Ph; R5 = C02Bn CONHMe S02Ph 65 G = Q-3; R6 = Me; R5 = Me Et n-Pr =Q-3;R6=Me;R5=i-Prc-Prn-Bu66G 67 G = Q-3; R6 = Me; R5 = i-Bu t-Bu n-Hex 68 G = Q-3; R6 = Me; R5 = c-Hex Bn CH2CH=CH2 69 G = Q-3; R6 = Me; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 70 G = Q-3; R6 = Me; R5 = CH2CN CH2CONH2 CH2CONHMe 71 G = Q-3 ; R6 = Me; R5 = CH2CONMe2 CH20Me CH20Bn 72 G = Q-3; R6 = Me; R5 = CH2SMe CH2S(O)Me CH2SO2Me 73 G = Q-3; R6 = Me; Rus = (CH2) 20H (CH2)2OMe (CH2) 2CF=CF2 74 G = Q-3; R6 = Me; R5 = OH OMe OEt 75 G = Q-3; R6 = Me; R5 = OBn OCH2C=CH OCH2-c-Pr 76 G = Q-3; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 77 G = Q-3; R6 = Me; R5 = COMe COEt COCF3 78 G = Q-3; R6 = Me; R5 = CO-i-Pr CO-c-Pr COPh 79 G = Q-3; R6 = Me; R5 = CH2CO2Me CO2Me CO2Et 80 G = Q-3; R6 =C02BnCONHMeS02Ph 81 G = Q-3; R6 = Ph; R5 = Me Et n-Pr 82 G = Q-3; R6 = Ph; R5 = i-Pr c-Pr n-Bu 83 G = Q-3; R6 = Ph; R5 = i-Bu t-Bu n-Hex 84 G = Q-3; R6 = Ph; R5 = c-Pen Bn CH2CH=CH2 =Q-3;85G Ph;R5=CH2CCl=CH2CH2C#CHCH2-c-Pr= =Q-3;86G Ph;R5=CH2CNCH2CONH2CH2CONHMe= =Q-3;87G Ph;R5=CH2CONMe2CH2OMeCH2OBn= 88 G = Q-3; R6 = Ph; R5 = CH2SMe CH2S(O)Me CH2SO2Me 89 G = Q-3; R6 = Ph; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 90 G = Q-3; R6 = Ph; R5 = OH OMe OEt =Q-3;91G Ph;R5=OBnOCH2C#CHOCH2-c-Pr= 92 G = Q-3; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 93 G = Q-3; R6 = Ph; R5 = COMe COEt COCF3 94 G = Q-3; R6 = Ph; R5 = CO-i-Pr CO-c-Pr COPh 95 G = Q-3; R6 = Ph; R5 = CH2CO2Me CO2Me CO2Et 96 G = Q-3; R6 = Ph; R5 = CO2Bn CONHMe SO2Ph TABLE 2 COLUMN 312 =Q-1;R6=COMe;R5=Eti-Prc-Pr1G 2 G = Q-1; R6 = COMe ; R5 = c-Hex Bn CH2C=CH 3 G = Q-1; R6 = COMe ; R5 = CH2CN CH2CONMe2 CH20Me 4 G = Q-1; R6 = COMe ; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 =Q-1;5G COMe;R5=OHOMeOBn= =Q-1;R6=COMe;R5=OCH2CNO(CH2)2CF=CF2CH2CO2Me6G 7 G = Q-1; R6 = CO-t-Bu; R5 = Me Et i-Pr 8 G = Q-1; R6 = CO-t-Bu; R5 = c-Pr n-Bu c-Hex 9 G = Q-1; R6 = CO-t-Bu; R5 = Bn Ph CH2C#CH 10 G = Q-1; R6 = CO-t-Bu; R5 = CH2CN CH2CONMe2 CH20Me 11 G = Q-1; R6 = CO-t-Bu; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 12 G = Q-1; R6 = CO-t-Bu; R5 = OH OMe OBn 13 G = Q-1 ; R6 = CO-t-Bu; R5 OCH2CN O (CH2) 2CF=CF2 CH2CO2Me =Q-1;R6=CO2Me;R5=Eti-Prc-Pr14G =Q-1;15G CO2Me;R5=c-HexBnCH2C#CH= 16 G = Q-1; R6 = C02Me ; R5 CH2CN CH2CONMe2 CH20Me 17 G = Q-1; R6 = CO2Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 =Q-1;18G CO2Me;R5=OHOMeOBn= =Q-1;19G CO2Me;R5=OCH2CNO(CH2)2CF=CF2CH2CO2Me= 20 G = Q-1; R6 = C02-t-Bu; R5 = Me Et i-Pr 21 G = Q-1; R6 = C02-t-Bu; R5 = c-Pr n-Bu c-Hex 22 G = Q-1 ; R6 = C02-t-Bu; R5 = Bn Ph CH2C=CH 23 G = Q-1; R6 = C02-t-Bu; R5 = CH2CN CH2CONMe2 CH20Me 24 G = Q-1; R6 = CO2-t-Bu ; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 25 G = Q-1; R6 = C02-t-Bu; R5 = OH OMe OBn 26 G = Q-1; R6 = C02-t-Bu; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 27 G = Q-1; R6 = CONMe2; R5 = Me Et i-Pr 28 G = Q-1; R6 = CONMe2; R5 = c-Pr n-Bu c-Hex 29 G = Q-1; R6 = CONMe2; R5 =BnPhCH2C=CH 30 G = Q-1; R6 = CONMe2; R5 = CH2CN CH2CONMe2 CH2OMe. 31 G = Q-1; R6 = CONMe2; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 32 G = Q-1; R6 = CONMe2; R5 = OH OMe OBn 33 G = Q-1; R6 = CONMe2; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 34 G = Q-1; R6 = S02Me; R5 = Me Et i-Pr 35 G = Q-1; R6 = S02Me; R5 = c-Pr n-Bu c-Hex 36 G = Q-1; R6 = S02Me; R5 = Bn Ph CH2C=CH 37 G = Q-1; R6 = S02Me; R5 = CH2CN CH2CONMe2 CH20Me 38 G = Q-1 ; R6 = S02Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 39 G = Q-1 ; R6 = S02Me; R5 = OH OMe OBn 40 G = Q-1 ; R6 = S02Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 41 G = Q-1 ; R6 = S02CF3; R5 = Me Et i-Pr 42 G = Q-1 ; R6 = S02CF3; R5 = c-Pr n-Bu c-Hex 43 G = Q-1 ; R6 = S02CF3; R5 = Bn Ph CH2C=CH 44 G = Q-1 ; R6 = S02CF3; R5 = CH2CN CH2CONMe2 CH2OMe 45 G = Q-1 ; R6 = S02CF3; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 46 G = Q-1 ; R6 = S02CF3; R5 = OH OMe OBn 47 G = Q-1 ; R6 = S02CF3; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 48 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = Me Et i-Pr 49 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = c-Pr n-Bu c-Hex 50 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = Bn Ph CH2C=CH 51 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = CH2CN CH2CONMe2 CH20Me 52 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 53 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = OH OMe OBn 54 G = Q-1 ; R6 = P (O) (OMe) 2; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 55 G = Q-1; R6 = P (O) (OMe) Me; R5 = Me Et i-Pr 56 G = Q-1 ; R6 = P (O) (OMe) Me; R5 = c-Pr n-Bu c-Hex 57 G = Q-1 ; R6 = P (O) (OMe) Me; R5 = Bn Ph CH2C=CH 58 G = Q-1 ; R6 = P (O) (OMe) Me; R5 = CH2CN CH2CONMe2 CH20Me 59 G = Q-1 ; R6 = P (O) (OMe) Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 60 G = Q-1 ; R6 = P (O) (OMe) Me; R5= OH OMe OBn 61 G = Q-1 ; R6 = P (O) (OMe) Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 62 G = Q-2 ; R6 = COMe; R5 = Et i-Pr c-Pr 63 G = Q-2 ; R6 = COMe; R5 = c-Hex Bn CH2C=CH 64 G = Q-2 ; R6 = COMe; R5 = CH2CN CH2CONMe2 CH20Me 65 G = Q-2 ; R6 = COMe; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 66 G = Q-2 ; R6 = COMe; R5 = OH OMe OBn 67 G = Q-2; R6 = COMe ; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 68 G = Q-2; R6 = CO-t-Bu; R5 = Me Et i-Pr 69 G = Q-2 ; R6 = CO-t-Bu; R5 = c-Pr n-Bu c-Hex 70 G = Q-2 ; R6 = CO-t-Bu; R5 = Bn Ph CH2C=CH 71 G = Q-2 ; R6 = CO-t-Bu; R5 = CH2CN CH2CONMe2 CH20Me 72 G = Q-2 ; R6 = CO-t-Bu; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 =Q-2;R6=CO-t-Bu;73G OHOMeOBn= 74 G = Q-2; R6 = CO-t-Bu; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 75 G = Q-2 ; R6 = C02Me; R5 = Et i-Pr c-Pr 76 G = Q-2 ; R6 = C02Me; R5 = c-Hex Bn CH2C=CH 77 G = Q-2 ; R6 = C02Me; R5 = CH2CN CH2CONMe2 CH20Me 78 G = Q-2; R6 = C02Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 79 G = Q-2; R6 = C02Me; R5 = OH OMe OBn 80 G = Q-2; R6 = C02Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 81 G = Q-2; R6 = C02-t-Bu; R5 = Me Et i-Pr 82 G = Q-2; R6 = C02-t-Bu; R5 = c-Pr n-Bu c-Hex 83 G = Q-2; R6 = C02-t-Bu; R5 = Bn Ph CH2C=CH 84 G = Q-2; R6 = C02-t-Bu; R5 = CH2CN CH2CONMe2 CH20Me 85 G = Q-2; R6 = C02-t-Bu; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 86 G = Q-2; R6 = C02-t-Bu; R5 = OH OMe OBn 87 G = Q-2; R6 = CO2-t-Bu ; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 88 G = Q-2; R6 = CONMe2; R5 = Me Et i-Pr 89 G = Q-2; R6 = CONMe2; R5 = c-Pr n-Bu c-Hex 90 G = Q-2; R6 = CONMe2; R5 = Bn Ph CH2C=CH 91 G = Q-2; R6 = CONMe2; R5 = CH2CN CH2CONMe2 CH20Me 92 G = Q-2; R6 = CONMe2; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 93 G = Q-2; R6 = CONMe2; R5 = OH OMe OBn 94 G = Q-2; R6 = CONMe2; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 95 G = Q-2; R6 = SO2Me ; R5 = Me Et i-Pr 96 G = Q-2; R6 = S02Me; R5 = c-Pr n-Bu c-Hex 97 G = Q-2; R6 = SO2Me; R5 = Bn Ph CH2C#CH 98 G = Q-2; R6 = S02Me; R5 = CH2CN CH2CONMe2 CH20Me 99 G = Q-2; R6 = S02Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 100 G = Q-2; R6 = S02Me; R5 = OH OMe OBn 101 G = Q-2; R6 = S02Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 102 G = Q-2; R6 = S02CF3; R5 = Me Et i-Pr 103 G = Q-2; R6 = S02CF3; R5 = c-Pr n-Bu c-Hex 104 G = Q-2; R6 = S02CF3; R5 = Bn Ph CH2C=CH 105 G = Q-2; R6 = S02CF3; R5 = CH2CN CH2CONMe2 CH20Me 106 G = Q-2; R6 = S02CF3; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 107 G = Q-2; R6 = S02CF3; R5= OH OMe OBn 108 G = Q-2; R6 = S02CF3; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 109 G = Q-2; R6 = P (O) (OMe) 2; R5 = Me Et i-Pr 110 G = Q-2; R6 = P (O) (OMe) 2; R5= c-Pr n-Bu c-Hex 111 G = Q-2; R6 = P (O) (OMe) 2; R5 = Bn Ph CH2C=CH 112 G = Q-2; R6 = P (O) (OMe) 2; R5 = CH2CN CH2CONMe2 CH20Me 113 G = Q-2; R6 = P (O) (OMe) 2; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 114 G = Q-2; R6 = P (O) (OMe) 2; R5 = OH OMe OBn 115 G = Q-2; R6 = P (O) (OMe) 2; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 116 G = Q-2; R6 = P (O) (OMe) Me; R5 = Me Et i-Pr 117 G = Q-2; R6 = P (O) (OMe) Me; R5 = c-Pr n-Bu c-Hex 118 G = Q-2; R6 = P (O) (OMe) Me; R5 = Bn Ph CH2C=CH 119 G = Q-2; R6 = P (O) (OMe) Me; R5 = CH2CN CH2CONMe2 CH20Me 120 G = Q-2; R6 = P (O) (OMe) Me; R5 = CH2SMe CH2S02Me (CH2) 2CF=CF2 121 G = Q-2; R6 = P (O) (OMe) Me; R5 = OH OMe OBn 122 G = Q-2; R6 = P (O) (OMe) Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 123 G = Q-3; R6 = COMe; R5 = Et i-Pr c-Pr 124 G = Q-3; R6 = COMe; R5 = c-Hex Bn CH2C#CH 125 G = Q-3; R6 = COMe; R5 = CH2CN CH2CONMe2 CH20Me 126 G = Q-3; R6 = COMe ; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 127 G = Q-3; R6 = COMe; R5 = OH OMe OBn 128 G = R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 129 G = Q-3; R6 = CO-t-Bu; R5 = Me Et i-Pr 130 G = Q-3; R6 = CO-t-Bu; R5 = c-Pr n-Bu c-Hex 131 G = Q-3; R6 = CO-t-Bu; R5 = Bn Ph CH2C=CH 132 G = Q-3; R6 = CO-t-Bu; R5 = CH2CN CH2CONMe2 CH20Me 133 G = Q-3; R6 = CO-t-Bu; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 134 G = Q-3; R6 = CO-t-Bu; R5 = OH OMe OBn 135 G = Q-3; R6 = CO-t-Bu; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 136 G = Q-3; R6 = C02Me; R5 = Et i-Pr c-Pr 137 G = Q-3; R6 = C02Me; R5 = c-Hex Bn CH2C=CH 138 G = Q-3; R6 = C02Me; R5 = CH2CN CH2CONMe2 CH20Me 139 G = Q-3; R6 = C02Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 140 G = Q-3; R6 = C02Me; R5 = OH OMe OBn 141 G = Q-3; R6 = C02Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 142 G = Q-3; R6 = C02-t-Bu; R5 = Me Et i-Pr 143 G = Q-3; R6 = C02-t-Bu; R5 = c-Pr n-Bu c-Hex 144 G = Q-3; R6 = C02-t-Bu; R5 = Bn Ph CH2C=CH 145 G = Q-3; R6 = C02-t-Bu; R5 = CH2CN CH2CONMe2 CH20Me 146 G = Q-3; R6 = C02-t-Bu; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 147 G = Q-3; R6 = C02-t-Bu; R5 = OH OMe OBn 148 G = Q-3; R6 = C02-t-Bu; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 149 G = Q-3; R6 = CONMe2; R5 = Me Et i-Pr 150 G = Q-3; R6 = CONMe2; R5 = c-Pr n-Bu c-Hex 151 G = Q-3; R6 = CONMe2; R5 = Bn Ph CH2C=CH 152 G = Q-3; R6 = CONMe2; R5 = CH2CN CH2CONMe2 CH20Me 153 G = Q-3; R6 = CONMe2; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 154 G = Q-3; R6 = CONMe2; R5 = OH OMe OBn 155 G = Q-3; R6 = CONMe2; R5= OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 156 G = Q-3; R6 = S02Me; R5 = Me Et i-Pr 157 G = Q-3; R6 = S02Me; R5 = c-Pr n-Bu c-Hex 158 G = Q-3; R6 = S02Me; R5 = Bn Ph CH2C-CH 159 G = Q-3; R6 = S02Me; R5 = CH2CN CH2CONMe2 CH20Me 160 G = Q-3; R6 = S02Me; R5 = CH2SMe CH2S02Me (CH2) 2CF=CF2 161 G = Q-3; R6 = S02Me; R5 = OH OMe OBn 162 G = Q-3; R6 = S02Me; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 163 G = Q-3; R6 = S02CF3; R5 = Me Et i-Pr 164 G = Q-3; R6 = S02CF3; R5 = c-Pr n-Bu c-Hex 165 G = Q-3; R6 = S02CF3; R5 = Bn Ph CH2C-CH 166 G = Q-3; R6 = S02CF3; R5 = CH2CN CH2CONMe2 CH20Me 167 G = Q-3; R6 = S02CF3; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 168 G = Q-3; R6 = S02CF3; R5 = OH OMe OBn 169 G = Q-3; R6 = S02CF3; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 170 G = Q-3; R6 = P (O) (OMe) 2; R5 = Me Et i-Pr 171 G = Q-3; R6 = P (O) (OMe) 2; R5 = c-Pr n-Bu c-Hex 172 G = Q-3; R6 = P (O) (OMe) 2; R5 = Bn Ph CH2C-CH 173 G = Q-3; R6 = P (O) (OMe) 2; R5 = CH2CN CH2CONMe2 CH20Me 174 G = Q-3; R6 = P (O) (OMe) 2; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 175 G = Q-3; R6 = P (O) (OMe) 2; R5 = OH OMe OBn 176 G = Q-3; R6 = P (O) (OMe) 2; R5 = OCH2CN O (CH2) 2CF=CF2 CH2CO2Me 177 G = Q-3; R6 = P (O) (OMe) Me; R5 = Me Et i-Pr 178 G = Q-3; R6 = P (O) (OMe) Me; R5 = c-Pr n-Bu c-Hex 179 G = Q-3; R6 = P (O) (OMe) Me; R5 = Bn Ph CH2C=CH 180 G = Q-3; R6 = P (O) (OMe) Me; R5 = CH2CN CH2CONMe2 CH20Me 181 G = Q-3; R6 = P (O) (OMe) Me; R5 = CH2SMe CH2SO2Me (CH2) 2CF=CF2 182 G = Q-3; R6 = P (O) (OMe) Me; R5 = OH OMe OBn 183 G = Q-3; R6 = P (O) (OMe) Me; R5 = OCH2CN O(CH2)2CF=CF2 CH2CO2Me TABLE 3 COLUMN 1 2 3 1 G = Q-1 ; R6 = 2-Pyr; R5 = Me Et n-Pr 2 G = Q-1 ; R6 = 2-Pyr; R5 = i-Pr c-Pr n-Bu 3 G = Q-1 ; R6 = 2-Pyr; R5 = i-Bu t-Bu n-Hex 4 G = Q-1 ; R6 = 2-Pyr; R5 = c-Pen Bn CH2CH=CH2 5 G = Q-1 ; R6 = 2-Pyr ; R5 = CH2CCl=cH2 CH2CCH CH2-c-Pr 6 G = Q-1 ; R6 = 2-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 7 G = Q-1 ; R6 = 2-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 8 G = Q-1 ; R6 = 2-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 9 G = Q-1 ; R6 = 2-Pyr; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 10 G = Q-1 ; R6 = 2-Pyr; R5 = OH OMe OEt 11 G = Q-1; R6 = 2-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 12 G = Q-1; R6 = 2-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 13 G = Q-1; R6 = 2-Pyr; R5 = COMe COEt COCF3 14 G = Q-1 ; R6 = 2-Pyr ; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 15 G = Q-1; R6 = 2-Pyr ; R5 = COPh CH2CO2Me CO2Me 16 G = Q-1; R6 = 2-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu =Q-1;R6=2-Pyr;R5=CO2BnCONHMeCONMe217G 18 G = Q-1; R6 = 2-Pyr; R5 = SO2Me SO2CF3 SO2Ph 19 G = Q-1; R6 = 2-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 20 G = Q-1; R6 = 3-Pyr; R5 = Me Et n-Pr 21 G = Q-1; R6 = 3-Pyr; R5 = i-Pr c-Pr n-Bu 22 G = Q-1 ; R6 = 3-Pyr; R5 = i-Bu t-Bu n-Hex 23 G = Q-1; R6 = 3-Pyr; R5 = c-Pen Bn CH2CH=CH2 24 G = Q-1; R6 = 3-Pyr; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 25 G = Q-1 ; R6 = 3-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 26 G = Q-1; R6 = 3-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 27 G = Q-1; R6 = 3-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 28 G = Q-1; R6 = 3-Pyr; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 29 G = Q-1; R6 = 3-Pyr; R5 = OH OMe OEt 30 G = Q-1; R6 = 3-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 31 G = Q-1; R6 = 3-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 32 G = Q-1; R6 = 3-Pyr; R5 = COMe COEt COCF3 33 G = Q-1 ; R6 = 3-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 34 G = Q-1; R6 = 3-Pyr; R5 = COPh CH2C02Me C02Me 35 G = Q-1; R6 = 3-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 36 G = Q-1; R6 = 3-Pyr; R5 = C02Bn CONHMe CONMe2 37 G = Q-1; R6 = 3-Pyr; R5 = S02Me S02CF3 S02Ph 38 G = Q-1; R6 = 3-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 39 G = Q-1 ; R6 = 4-Pyr; R5 = Me Et n-Pr 40 G = Q-1; R6 = 4-Pyr; R5 = i-Pr c-Pr n-Bu 41 G = Q-1; R6 = 4-Pyr; R5 = i-Bu t-Bu n-Hex 42 G = Q-1; R6 = 4-Pyr ; R5 = c-Pen Bn CH2CH=CH2 43 G = Q-1; R6 = 4-Pyr; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 44 G = Q-1; R6 = 4-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 45 G = Q-1 ; R6 = 4-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 46 G = Q-1; R6 = 4-Pyr; R5 = CH2SMe CH2S(O)Me CH2SO2Me 47 G = Q-1; R6 = 4-Pyr; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 48 G = Q-1; R6 = 4-Pyr; R5 = OH OMe OEt 49 G = Q-1; R6 = 4-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 50 G = Q-1 ; R6 = 4-Pyr ; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 51 G = Q-1 ; R6 = 4-Pyr; R5 = COMe COEt COCF3 52 G = Q-1 ; R6 = 4-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 53 G = Q-1 ; R6 = 4-Pyr; R5 = COPh CH2CO2Me C02Me =Q-1;R6=4-Pyr;R5=CO2EtCO2-i-PrCO2-t-Bu54G =Q-1;55G R6 R5=CO2BnCONHMeCONMe24-Pyr; =Q-1;R6=4-Pyr;R5=SO2MeSO2CF3SO2Ph56G 57 G = Q-1 ; R6 = 4-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 58 G = Q-1 ; R6 = 2-Th; R5 = Me Et n-Pr 59 G = Q-l ; R6 = 2-Th; R5= i-Pr c-Pr n-Bu 60 G = Q-1 ; R6 = 2-Th; R5 = i-Bu t-Bu n-Hex 61 G = Q-1 ; R6 = 2-Th; R5 = c-Pen Bn CH2CH=CH2 62 G = Q-1 ; R6 = 2-Th; R5 = CH2CCl=CH2 CH2C=CH CH2-c-Pr 63 G = Q-1 ; R6 = 2-Th; R5 = CH2CN CH2CONH2 CH2CONHMe 64 G = Q-1 ; R6 = 2-Th; R5 = CH2CONMe2 CH20Me CH20Bn 65 G = Q-1 ; R6 = 2-Th; R5 = CH2SMe CH2S (O) Me CH2SO2Me 66 G = Q-1 ; R6 = 2-Th; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 67 G = Q-1 ; R6 = 2-Th; R5 = OH OMe OEt 68 G = Q-1 ; R6 = 2-Th; R5 = OBn OCH2C=CH OCH2-c-Pr 69 G = Q-1 ; R6 = 2-Th; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 70 G = Q-1 ; R6 = 2-Th; R5 = COMe COEt COCF3 71 G = Q-1 ; R6 = 2-Th; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 72 G = Q-1 ; R6 = 2-Th; R5 = COPh CH2C02Me C02Me 73 G = Q-1 ; R6 = 2-Th; R5 = C02Et C02-i-Pr C02-t-Bu 74 G = Q-1 ; R6 = 2-Th; R5 = C02Bn CONHMe CONMe2 75 G = Q-1 ; R6 = 2-Th; R5 = S02Me S02CF3 S02Ph 76 G = Q-1 ; R6 = 2-Th; R5= P (O) (OMe) 2 P (O) (OMe) Me Ph 77 G = Q-2; R6 = 2-Pyr; R5 = Me Et n-Pr 78 G = Q-2 ; R6 = 2-Pyr; R5 = i-Pr c-Pr n-Bu 79 G = Q-2 ; R6 = 2-Pyr; R5 = i-Bu t-Bu n-Hex 80 G = Q-2; R6 = 2-Pyr; R5 = c-Pen Bn CH2CH=CH2 81 G = Q-2; R6 = 2-Pyr; R5 =CH2CC1=CH2CH2C=CHCH2-c-Pr 82 G = Q-2 ; R6 = 2-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 83 G = Q-2; R6 = 2-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 84 G = Q-2; R6 = 2-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 85 G = Q-2; R6 = 2-Pyr; R5 = (CH2) 20H (CH2) 2OMe (CH2) 2CF=CF2 86 G = Q-2; R6 = 2-Pyr; R5 = OH OMe OEt 87 G = Q-2 ; R6 = 2-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 88 G = Q-2; R6 = 2-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 89 G = Q-2 ; R6 = 2-Pyr; R5 = COMe COEt COCF3 90 G = Q-2; R6 = 2-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 91 G = Q-2; R6 = 2-Pyr; R5 = COPh CH2CO2Me C02Me 92 G = Q-2; R6 = 2-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 93 G = Q-2; R6 = 2-Pyr; R5 = C02Bn CONHMe CONMe2 94 G = Q-2; R6 = 2-Pyr; R5 = S02Me S02CF3 S02Ph 95 G = Q-2; R6 = 2-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 96 G = Q-2; R6 = 3-Pyr; R5 = Me Et n-Pr 97 G = Q-2; R6 = 3-Pyr; R5 = i-Pr c-Pr n-Bu 98 G = Q-2; R6 = 3-Pyr; R5 = i-Bu t-Bu n-Hex 99 G = Q-2; R6 = 3-Pyr; R5 = c-Pen Bn CH2CH=CH2 100 G = Q-2; R6 = 3-Pyr; R5 = CH2CCl=cH2 CH2CCH CH2-c-Pr 101 G = Q-2; R6 = 3-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 102 G = Q-2; R6 = 3-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 103 G = Q-2; R6 = 3-Pyr; R5 = CH2SMe CH2S(O)Me CH2SO2Me 104 G = Q-2; R6 = 3-Pyr; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 105 G = Q-2; R6 = 3-Pyr; R5 = OH OMe OEt 106 G = Q-2; R6 = 3-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 107 G = Q-2; R6 = 3-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 108 G = Q-2; R6 = 3-Pyr; R5 = COMe COEt COCF3 109 G = Q-2; R6 = 3-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 110 G = Q-2; R6 = 3-Pyr; R5 = COPh CH2C02Me C02Me 111 G = Q-2; R6 = 3-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 112 G = Q-2; R6 = 3-Pyr; R5 = C02Bn CONHMe CONMe2 113 G = Q-2; R6 = 3-Pyr; R5 = S02Me S02CF3 S02Ph 114 G = Q-2; R6 = 3-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 115 G = Q-2; R6 = 4-Pyr; R5 = Me Et n-Pr 116 G = Q-2; R6 = 4-Pyr; R5 = i-Pr c-Pr n-Bu 117 G = Q-2; R6 = 4-Pyr; R5 = i-Bu t-Bu n-Hex 118 G = Q-2; R6 = 4-Pyr; R5 = c-Pen Bn CH2CH=CH2 119 G = Q-2; R6 = 4-Pyr; R5 = CH2CCl=cH2 CH2CCH CH2-c-Pr 120 G = Q-2; R6 = 4-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 121 G = Q-2; R6 = 4-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 122 G = Q-2; R6 = 4-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 123 G = Q-2; R6 = 4-Pyr; R5 = (CH2) 20H (CH2) 2OMe (CH2) 2CF=CF2 124 G = Q-2; R6 = 4-Pyr; R5 = OH OMe OEt 125 G = Q-2; R6 = 4-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 126 G = Q-2; R6 = 4-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 127 G = Q-2; R6 = 4-Pyr; R5 = COMe COEt COCF3 128 G = Q-2; R6 = 4-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 129 G = Q-2; R6 = 4-Pyr; R5 = COPh CH2C02Me C02Me 130 G = Q-2; R6 = 4-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 131 G = Q-2; R6 = 4-Pyr; R5 = C02Bn CONHMe CONMe2 132 G = Q-2; R6 = 4-Pyr; R5 = SO2Me SO2CF3 SO2Ph 133 G = Q-2; R6 = 4-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 134 G = Q-2; R6 = 2-Th; R5 = Me Et n-Pr 135 G = Q-2; R6 = 2-Th; R5 = i-Pr c-Pr n-Bu 136 G = Q-2; R6 = 2-Th; R5 = i-Bu t-Bu n-Hex 137 G = Q-2; R6 = 2-Th; R5 = c-Pen Bn CH2CH=CH2 138 G = Q-2; R6 = 2-Th; R5 = CH2CCl=CH2 CH2C=CH CH2-c-Pr 139 G = Q-2; R6 = 2-Th; R5 = CH2CN CH2CONH2 CH2CONHMe 140 G = Q-2; R6 = 2-Th; R5 = CH2CONMe2 CH20Me CH20Bn 141 G = Q-2; R6 = 2-Th; R5 = CH2SMe CH2S (O) Me CH2SO2Me 142 G = Q-2; R6 = 2-Th; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 143 G = Q-2; R6 = 2-Th; R5 = OH OMe OEt 144 G = Q-2; R6 = 2-Th; R5 = OBn OCH2C=CH OCH2-c-Pr 145 G = Q-2; R6 = 2-Th; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 146 G = Q-2; R6 = 2-Th; R5 = COMe COEt COCF3 147 G = Q-2; R6 = 2-Th; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 148 G = Q-2; R6 = 2-Th; R5 = COPh CH2CO2Me C02Me 149 G = Q-2; R6 = 2-Th; R5 = C02Et C02-i-Pr C02-t-Bu 150 G = Q-2; R6 = 2-Th; R5 = C02Bn CONHMe CONMe2 151 G = Q-2; R6 = 2-Th; R5 = S02Me S02CF3 S02Ph 152 G = Q-2; R6 = 2-Th; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 153 G = Q-3; R6 = 2-Pyr; R5 = Me Et n-Pr 154 G = Q-3; R6 = 2-Pyr; R5 = i-Pr c-Pr n-Bu 155 G = Q-3; R6 = 2-Pyr; R5 = i-Bu t-Bu n-Hex 156 G = Q-3; R6 = 2-Pyr; R5 = c-Pen Bn CH2CH=CH2 157 G = Q-3; R6 = 2-Pyr; R5 = CH2CCI=CH2 CH2C=CH CH2-c-Pr 158 G = Q-3; R6 = 2-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 159 G = Q-3; R6 = 2-Pyr; R5 = CH2CONMe2 CH20Me CH20Bn 160 G = Q-3; R6 = 2-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 161 G = Q-3; R6 = 2-Pyr; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 162 G = Q-3; R6 = 2-Pyr; R5 = OH OMe OEt 163 G = Q-3; R6 = 2-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 164 G = Q-3; R6 = 2-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 165 G = Q-3; R6 = 2-Pyr; R5 = COMe COEt COCF3 166 G = Q-3; R6 = 2-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 167 G = Q-3; R6 = 2-Pyr; R5 = COPh CH2C02Me C02Me 168 G = Q-3; R6 = 2-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 169 G = Q-3; R6 = 2-Pyr; R5 = CO2Bn CONHMe CONMe2 170 G = Q-3; R6 = 2-Pyr; R5 = S02Me S02CF3 S02Ph 171 G = Q-3; R6 = 2-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 172 G = Q-3; R6 = 3-Pyr; R5 = Me Et n-Pr 173 G = Q-3; R6 = 3-Pyr; R5 = i-Pr c-Pr n-Bu 174 G = Q-3; R6 = 3-Pyr; R5 = i-Bu t-Bu n-Hex 175 G = Q-3; R6 = 3-Pyr; R5 = c-Pen Bn CH2CH=CH2 176 G = Q-3; R6 = 3-Pyr; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 177 G = Q-3; R6 = 3-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 178 G = Q-3; R6 = 3-Pyr; R5= CH2CONMe2 CH20Me CH20Bn 179 G = Q-3; R6 = 3-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 180 G = Q-3; R6 = 3-Pyr; R5 = (CH2) 20H (CH2) 2OMe (CH2) 2CF=CF2 181 G = Q-3; R6 = 3-Pyr; R5 = OH OMe OEt 182 G = Q-3; R6 = 3-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 183 G = Q-3; R6 = 3-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 184 G = Q-3; R6 = 3-Pyr; R5 = COMe COEt COCF3 185 G = Q-3; R6 = 3-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 186 G = Q-3; R6 = 3-Pyr; R5 = COPh CH2CO2Me C02Me 187 G = Q-3; R6 = 3-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 188 G = Q-3; R6 = 3-Pyr; R5 = C02Bn CONHMe CONMe2 189 G = Q-3; R6 = 3-Pyr; R5= S02Me S02CF3 S02Ph 190 G = Q-3; R6 = 3-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 191 G = Q-3; R6 = 4-Pyr; R5 = Me Et n-Pr 192 G = Q-3; R6 = 4-Pyr; R5 = i-Pr c-Pr n-Bu 193 G = Q-3; R6 = 4-Pyr; R5 = i-Bu t-Bu n-Hex 194 G = Q-3; R6 = 4-Pyr; R5 = c-Pen Bn CH2CH=CH2 195 G = Q-3; R6 = 4-Pyr; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 196 G = Q-3; R6 = 4-Pyr; R5 = CH2CN CH2CONH2 CH2CONHMe 197 G = R5 = CH2CONMe2 CH20Me CH20Bn 198 G = Q-3; R6 = 4-Pyr; R5 = CH2SMe CH2S (O) Me CH2SO2Me 199 G = Q-3; R6 = 4-Pyr; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 200 G = Q-3; R6 = 4-Pyr; R5= OH OMe OEt 201 G = Q-3; R6 = 4-Pyr; R5 = OBn OCH2C=CH OCH2-c-Pr 202 G = Q-3; R6 = 4-Pyr; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 203 G = R5 = COMe COEt COCF3 204 G = Q-3; R6 = 4-Pyr; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 205 G = Q-3; R6 = 4-Pyr; R5 = COPh CH2C02Me C02Me 206 G = Q-3; R6 = 4-Pyr; R5 = C02Et C02-i-Pr C02-t-Bu 207 G = Q-3; R6 = 4-Pyr; R5 = CO2Bn CONHMe CONMe2 208 G = Q-3; R6 = 4-Pyr; R5 = S02Me S02CF3 S02Ph 209 G = Q-3; R6 = 4-Pyr; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 210 G = Q-3; R6 = 2-Th; R5 = Me Et n-Pr 211 G = Q-3; R6 = 2-Th; R5 = i-Pr c-Pr n-Bu 212 G = Q-3; R6 = 2-Th; R5 = i-Bu t-Bu n-Hex 213 G = Q-3; R6 = 2-Th; R5 = c-Pen Bn CH2CH=CH2 214 G = Q-3; R6 = 2-Th; R5 = CH2CC1=CH2 CH2C=CH CH2-c-Pr 215 G = Q-3; R6 = 2-Th; R5 = CH2CN CH2CONH2 CH2CONHMe 216 G = Q-3; R6 = 2-Th; R5 = CH2CONMe2 CH20Me CH20Bn 217 G = Q-3; R6 = 2-Th; R5 = CH2SMe CH2S (O) Me CH2SO2Me 218 G = Q-3; R6 = 2-Th; R5 = (CH2) 20H (CH2) 20Me (CH2) 2CF=CF2 219 G = Q-3; R6 = 2-Th; R5 = OH OMe OEt 220 G = Q-3; R6 = 2-Th; R5 = OBn OCH2C=CH OCH2-c-Pr 221 G = Q-3; R6 = 2-Th; R5 = OCH2CN O (CH2) 2CF=CF2 CHO 222 G = Q-3; R6 = 2-Th; R5 = COMe COEt COCF3 223 G = Q-3; R6 = 2-Th; R5 = CO-i-Pr CO-c-Pr CO-t-Bu 224 G = Q-3; R6 = 2-Th; R5 = COPh CH2CO2Me C02Me 225 G = Q-3; R6 = 2-Th; R5 = C02Et C02-i-Pr C02-t-Bu 226 G = Q-3; R6 = 2-Th; R5 = C02Bn CONHMe CONMe2 227 G = Q-3; R6 = 2-Th; R5 = S02Me S02CF3 S02Ph 228 G = Q-3; R6 = 2-Th; R5 = P (O) (OMe) P (O) (OMe) Me Ph TABLE 4 COLUMN 1 2 3 4 1 G = Q-1; R5 = Me ; R17 = 2-F 3-F 4-F 2-Cl 2 G = Q-1; R5 = Me; R17 = 3-CI 4-CI 3-Br 4-Br 3 G = Q-1; R5 = Me ; R17 =3-14-13-Me4-Me =Q-1;R5=Me;4G 4-Et4-n-Pr4-i-Pr4-n-Bu= =Q-1;R5=Me;R17=4-t-Bu2,4-diCl2,6-diCl3,4-diCl5G 6 G = Q-1; R5 = Me; R17 = 3-CF3 4-CF3 3-CN 4-CN 7 G = Q-1; R5 = Me; R17 = 3-NO2 4-NO2 3-OH 4-OH 8 G = Q-1; R5 = Me; R17 = 3-OMe 4-OMe 4-OEt 4-O-t-Bu =Q-1;R5=Me;R17=3-SMe4-SMe3-OCF34-OCF39G 10 G = Q-1; R5 = Me; R17 = 3-S(O)Me 4-S(O)Me 3-SO2Me 4-SO2Me 11 G = Q-1; R5 = (CH2) 2CF=CF2; R1 2-F 3-F 4-F 2-Cl =Q-1;12G (CH2)2CF=CF2;R17=3-Cl4-Cl3-Br4-Br= 13 G = Q-1; R5 = (CH2) 2CF=CF2; R17 =3-14-13-Me4-Me =Q-1;14G (CH2)2CF=CF2;R17=4-Et4-n-Pr4-i-Pr4-n-Bu= =Q-1;15G (CH2)2CF=CF2;R17=4-t-Bu2,4-diCl2,6-diCl3,4-diCl= =Q-1;16G (CH2)2CF=CF2;R17=3-CF34-CF33-CN4-CN= 17 G = Q-1; R5 = (CH2) 2CF=CF2; R17= 3-NO2 4-NO2 3-OH 4-OH =Q-1;R5=(CH2)2CF=CF2;R17=3-OMe4-OMe4-OEt4-O-t-Bu18G 19 G = Q-1; R5 = (CH2) 2CF=CF2; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 =Q-1;20G (CH2)2CF=CF2R17=3-S(O)Me4-S(O)Me3-SO2Me4-SO2Me= =Q-1;21G CO2Me;R17=2-F3-F4-F2-Cl= =Q-1;R5=CO2Me;R17=3-Cl4-Cl3-Br4-Br22G =Q-1;R5=CO2Me;R17=3-I4-I3-Me4-Me23G =Q-1;R5=CO2Me;R17=4-Et4-n-Pr4-i-Pr4-n-Bu24G =Q-1;25G CO2Me;R17=4-t-Bu2,4-diCl2,6-diCl3,4-diCl= 26 G = Q-1 ; R5 = CO2Me ; R17 = 3-CF3 4-CF3 3-CN 4-CN =Q-1;R5=CO2Me;R17=3-NO24-NO23-OH4-OH27G =Q-1;R5=CO2Me;R17=3-OMe4-OMe4-OEt4-O-t-Bu28G =Q-1;29G CO2Me;R17=3-SMe4-SMe3-OCF34-OCF3= =Q-1;R5=CO2Me;R17=3-S(O)Me4-S(O)Me3-SO2Me4-SO2Me30G 31 G = Q-2; R5 = Me; R17 = 2-F 3-F 4-F 2-C1 =O-2;R5=Me;R17=3-Cl4-Cl3-Br4-Br32G 33 G = Q-2; R5 = Me; R1 =3-14-13-Me4-Me 34 G = Q-2 ; R5 = Me ; R17 = 4-Et 4-n-Pr 4-i-Pr 4-n-Bu =Q-2;35G Me;R17=4-t-Bu2,4-diCl2,6-diCl3,4-diCl= 36 G = Q-2; R5 = Me; R17 = 3-CF3 4-CF3 3-CN 4-CN 37 G = Q-2; R5 = Me; R17 = 3-NO2 4-NO2 3-OH 4-OH =Q-2;38G Me;R17=3-OMe4-OMe4-OEt4-O-t-Bu= 39 G = Q-2; R5 = Me; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 =Q-2;40G Me;R17=3-S(O)Me4-S(O)Me3-SO2Me4-SO2Me= 41 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 2-F 3-F 4-F 2-Cl 42 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-Cl 4-Cl 3-Br 4-Br 43 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-I 4-I 3-Me 4-Me 44 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 4-Et 4-n-Pr 4-i-Pr 4-n-Bu 45 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 4-t-Bu 2, 4-diCl 2, 6-diCl 3, 4-diCl 46 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-CF3 4-CF3 3-CN 4-CN 47 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-NO2 4-NO2 3-OH 4-OH 48 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-OMe 4-OMe 4-OEt 4-O-t-Bu 49 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 50 G = Q-2; R5 = (CH2) 2CF=CF2; R17 = 3-S(O)Me 4-S(O)Me 3-SO2Me 4-SO2Me 51 G = Q-2; R5 = C02Me; R17 = 2-F 3-F 4-F 2-Cl 52 G = Q-2; R5 = C02Me; R17 = 3-Cl 4-Cl 3-Br 4-Br 53 G = Q-2; R5 = C02Me; R17 = 3-I 4-I 3-Me 4-Me 54 G = Q-2; R5 = C02Me; R17 = R-Et 4-n-Pr 4-i-Pr 4-n-Bu 55 G = Q-2; R5 = C02Me; R17 = 4-t-Bu 2,4-diCl 2,6-diCl 3,4-diCl 56 G = Q-2; R5 = C02Me; R17 = 3-CF3 4-CF3 3-CN 4-CN 57 G = Q-2; R5 = C02Me; R17 = 3-N02 4-N02 3-OH 4-OH 58 G = Q-2; R5 = C02Me; R17 = 3-OMe 4-OMe 4-OEt 4-O-t-Bu 59 G = Q-2; R5 = C02Me; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 60 G = Q-2; R5 = C02Me; R17 = 3-S (O) Me 4-S (O) Me 3-SO2Me 4-SO2Me 61 G = Q-3; R5 = Me; R17 = 2-F 3-F 4-F 2-Cl 62 G = Q-3; R5 = Me; R17 = 3-Cl 4-Cl 3-Br 4-Br 63 G = Q-3; R5 = Me; R17 =3-14-13-Me4-Me 64 G = Q-3 ; R5 = Me ; R17 = 4-Et 4-n-Pr 4-i-Pr 4-n-Bu 65 G = Q-3; R5 = Me; R17 = 4-t-Bu 2, 4-diCl 2, 6-diCl 3, 4-diCl 66 G = Q-3 ; R5 = Me; R17 = 3-CF3 4-CF3 3-CN 4-CN 67 G = Q-3; R5 = Me; R17 = 3-N02 4-N02 3-OH 4-OH 68 G = Q-3; R5 = Me; R17 = 3-OMe 4-OMe 4-OEt 4-O-t-Bu 69 G = Q-3; R5 = Me; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 70 G = Q-3; R5 = Me; R17 = 3-S(O)Me 4-S(O)Me 3-SO2Me 4-SO2Me 71 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 2-F 3-F 4-F 2-Cl 72 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-CI 4-CI 3-Br 4-Br 73 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-I 4-I 3-Me 4-Me 74 G = Q-3; R5 = (CH2) 2CF=CF2; R17= 4-Et 4-n-Pr 4-i-Pr 4-n-Bu 75 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 4-t-Bu 2,4-diCl 2,6-diCl 3,4-diCl 76 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-CF3 4-CF3 3-CN 4-CN 77 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-NO2 4-NO2 3-OH 4-OH 78 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-OMe 4-OMe 4-OEt 4-O-t-Bu 79 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 80 G = Q-3; R5 = (CH2) 2CF=CF2; R17 = 3-S(O)Me 4-S(O)Me 3-SO2Me 4-SO2Me 81 G = Q-3; R5 = CO2Me; R17 = 2-F 3-F 4-F 2-Cl 82 G = Q-3; R5 = CO2Me; R17 = 3-Cl 4-Cl 3-Br 4-Br 83 G = Q-3; R5 = C02MeR3-14-13-Me4-Me 84 G = Q-3; R5 = CO2Me ; R17 = 4-Et 4-n-Pr 4-i-Pr 4-n-Bu 85 G = Q-3; R5 = CO2Me; R17 = 4-t-Bu 2,4-diCl 2,6-diCl 3,4-diCl 86 G = Q-3; R5 = CO2Me; R17 = 3-CF3 4-CF3 3-CN 4-CN 87 G = Q-3; R5 = CO2Me; R17 = 3-NO2 4-NO2 3-OH 4-OH 88 G = Q-3; R5 = CO2Me; R17 = 3-OMe 4-OMe 4-OEt 4-O-t-Bu 89 G = Q-3; R5 = CO2Me ; R17 = 3-SMe 4-SMe 3-OCF3 4-OCF3 90 G = Q-3; R5 = CO2Me; R17 = 3-S(O)Me 4-S(O)Me 3-SO2Me 4-SO2Me TABLE 5 (R2 = Et) COLUMN 1 2 3 1 R3 = Br; R6 = Me; R5 = Me i-Pr c-Pr 2 R3 = Br ; R6 = Me; R5 = t-Bu c-Hex Bn 3 R3 = Br; R6 = Me; R5 = CH2CN CH20Me CH2SO2Me 4 R3 = Br ; R6 = Me (CH2) 2CF=CF2 5 R3 = Br ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 6 R3 = Br ; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 7 R3 = Br ; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 8 R3 = Br ; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 9 R3 = Br; R6 = Ph ; R5 = Me Et i-Pr 10 R3 = Br ; R6 = Ph; R5 = c-Pr c-Pen Bn =Br;R6=Ph;11R3 CH2CNCH2OMeCH2SO2Me= =Br;12R3 Ph;R5=OHOMe(CH2)2CF=CF2= 13 R3 = Br ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 14 R3 = Br ; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 15 R3 = Br; R6 = Ph ; R5 = C02-t-Bu CONMe2 S02Me 16 R3 = Br; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 17 R3 = Me; R6 = Me ; R5 = Me i-Pr c-Pr 18 R3 = Me; R6 = Me ; R5 = t-Bu c-Hex Bn 19 R3 = Me; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 20 R3 = Me ; R6 = Me (CH2) 2CF=CF2 21 R3 = Me; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 22 R3 = Me ; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 23 R3 = Me; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 24 R3 = Me ; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 25 R3 = Me; R6 = Ph; R5 = Me Et i-Pr 26 R3 = Me; R6 = Ph; R5 = c-Pr c-Pen Bn 27 R3 = Me ; R6 = Ph; R5 = CH2CN CH20Me CH2S02Me 28 R3 = Me ; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 29 R3 = Me; R6 = Ph; R5= OCH2CN O (CH2) 2CF=CF2 COMe 30 R3 = Me; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 31 R3 = Me ; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 32 R3 = Me ; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 33 R3 = OMe; R6 = Me; R5 = Me i-Pr c-Pr 34 R3 = OMe; R6 = Me; R5 = t-Bu c-Hex Bn 35 R3 = OMe; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 36 R3 = OMe; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 37 R3 = OMe; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 38 R3 = OMe; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 39 R3 = OMe; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 40 R3 = OMe; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 41 R3 = OMe; R6 = Ph; R5 = Me Et i-Pr 42 R3 = OMe; R6 = Ph; R5 = c-Pr c-Pen Bn 43 R3 = OMe; R6 = Ph; R5 = CH2CN CH20Me CH2S02Me 44 R3 = OMe; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 45 R3 = OMe; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 46 R3 = OMe; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 47 R3 = OMe; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 48 R3 = OMe; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 49 R3 = SMe; R6 = Me; R5 = Me i-Pr c-Pr 50 R3 = SMe; R6 = Me; R5 = t-Bu c-Hex Bn 51 R3 = SMe; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 52 R3 = SMe; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 53 R3 = SMe; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 54 R3 = SMe; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 55 R3 = SMe; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 56 R3 = SMe; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 57 R3 = SMe; R6 = Ph; R5 = Me Et i-Pr 58 R3 = SMe; R6 = Ph; R5 = c-Pr c-Pen Bn 59 R3 = SMe; R6 = Ph; R5 = CH2CN CH20Me CH2S02Me 60 R3 = SMe; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 61 R3 = SMe; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 62 R3 = SMe; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 63 R3 = SMe; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 64 R3 = SMe; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 65 R3 = CN; R6 = Me; R5 = Me i-Pr c-Pr 66 R3 = CN; R6 = Me ; R5 = t-Bu c-Hex Bn 67 R3 = CN; R6 = Me; R5 = CH2CN CH2OMe CH2SO2Me 68 R3 = CN ; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 69 R3 = CN ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 70 R3 = CN ; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 71 R3 = CN ; R6 = Me 72 R3 = CN; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me =CN;73R3 Ph;R5=MeEti-Pr= 74 R3 = CN; R6 = Ph; R5 = c-Pr c-Pen Bn 75 R3 = CN; R6 = Ph; R5 = CH2CN CH2OMe CH2SO2Me 76 R3 = CN; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 77 R3 = CN ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =CN;78R3 Ph;R5=CO-t-BuCH2CO2MeCO2Me= 79 R3 = CN ; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 80 R3 = CN; R6 = Ph ; RS = SO CF P (O) (OMe) P (O) (OMe) Me TABLE 6 (R2 = CH20Me) COLUMN 1 2 3 1 R3 = Br ; R6 = Me ; R5 = Me i-Pr c-Pr 2 R3 = Br ; R6 = Me; R5 = t-Bu c-Hex Bn 3 R3 = Br ; R6 = Me; R5 = CH2CN CH20Me CH2SO2Me 4 R3 = Br ; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 5 R3 = Br ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 6 R3 = Br; R6 = Me; R5 = CO-t-Bu CH2CO2Me CO2Me 7 R3 = Br ; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 8 R3 = Br ; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 9 R3 = Br; R6 = Ph; R5 = Me Et i-Pr 10 R3 = Br ; R6 = Ph; R5 = c-Pr c-Pen Bn 11 R3 = Br ; R6 = Ph; R5 = CH2CN CH20Me CH2SO2Me 12 R3 = Br; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 13 R3 = Br; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 14 R3 = Br; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 15 R3 = Br ; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 16 R3 = Br; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 17 R3 = Me; R6 = Me; R5 = Me i-Pr c-Pr 18 R3 = Me; R6 = Me ; R5 = t-Bu c-Hex Bn 19 R3 = Me ; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 20 R3 = Me; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 21 R3 = Me; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 22 R3 = Me ; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 23 R3 = Me ; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 24 R3 = Me; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 25 R3 = Me; R6 = Ph ; R5 = Me Et i-Pr 26 R3 = Me; R6 = Ph; R5 = c-Pr c-Pen Bn 27 R3 = Me ; R6 = Ph; R5 = CH2CN CH20Me CH2S02Me 28 R3 = Me ; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 29 R3 = Me ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 30 R3 = Me ; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 31 R3 = Me ; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 32 R3 = Me ; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 33 R3 = SMe; R6 = Me; R5 = Me i-Pr c-Pr 34 R3 = SMe; R6 = Me; R5 = t-Bu c-Hex Bn 35 R3 = SMe; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 36 R3 = SMe; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 37 R3 = SMe; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 38 R3 = SMe; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 39 R3 = SMe; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 40 R3 = SMe; R6 = Me; R5= S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 41 R3 = SMe; R6 = Ph; R5 = Me Et i-Pr 42 R3 = SMe; R6 = Ph; R5 = c-Pr c-Pen Bn 43 R3 = SMe; R6 = Ph; R5 = CH2CN CH2OMe CH2SO2Me 44 R3 = SMe; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 45 R3 = SMe; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 46 R3 = SMe; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 47 R3 = SMe; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 48 R3 = SMe; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 49 R3 = CN; R6 = Me; R5 = Me i-Pr c-Pr 50 R3 = CN; R6 = Me ; R5 = t-Bu c-Hex Bn 51 R3 = CN ; R6 = Me; R5 = CH2CN CH20Me CH2S02Me =CN;52R3 Me;= R5 OMe(CH2)2CF=CF2OH =CN;R6=Me;53R3 R5 O(CH2)2CF=CF2COMeOCH2CN 54 R3 = CN ; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me =CN;R6=Me;55R3 CO2-t-BuCONMe2SO2Me= 56 R3 = CN ; R6 = Me; R5 = SO2CF3 P(O) (OMe) 2 P (O) (OMe) Me 57 R3 = CN; R6 = Ph; R5 = Me Et i-Pr 58 R3 = CN; R6 = Ph; R5 = c-Pr c-Pen Bn =CN;R6=Ph;59R3 CH2CNCH2OMeCH2SO2Me= 60 R3 = CN; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 =CN;R6=Ph;61R3 OCH2CNO(CH2)2CF=CF2COMe= 62 R3 = CN ; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 63 R3 = CN ; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 64 R3 = CN; R6 = Ph; R5 = SO2CF3 P(O) (OMe) 2 P (O) (OMe) Me TABLE 7 (R2 = Me) COLUMN 312 =Cl;1R3 Me:R5=Mei-Prc-Pr= 2 R3 = Cl ; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 3 R3 = Cl; R6 = Me ; R5 = CH2CO2Me OH OMe 4 R3 = Cl; R5 =OCH2CN0 (CH2) 2CF=CF2 COMe 5 R3 = Cl; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 6 R3 = Cl; R6 = Me ; R5= CONMe2 S02CF3 P (O) (OMe) Me =Cl;7R3 Ph;R5=MeEtc-Pr= 8 R3 = Cl ; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 9 R3 = Cl; R6 = Ph; R5 = CH2CO2Me OH OMe =Cl;R6=Ph;10R3 OCH2CNO(CH2)2CF=CF2COMe= 11 R3 = Cl ; R6 = Ph; RS = CO-t-Bu C02Me C02-t-Bu 12 R3 = Cl; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 13 R3 = Br; R6 = Me ; R5 = Me i-Pr c-Pr 14 R3 = Br; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 15 R3 = Br ; R6 = Me; R5 = CH2CO2Me OH OMe 16 R3 = Br ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 17 R3 = Br; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 18 R3 = Br ; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 19 R3 = Br; R6 = Ph ; R5 = Me Et c-Pr 20 R3 = Br; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 21 R3 = Br; R6 = Ph; R5 = CH2CO2Me OH OMe 22 R3 = Br ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 23 R3 = Br ; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 24 R3 = Br; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 25 R3 = Me; R6 = Me; R5 = Me i-Pr c-Pr 26 R3 = Me; R6 = Me ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 R3 = Me; R6 = Me; R5 = CH2CO2Me OH OMe 28 R3 = Me ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 R3 = Me ; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 30 R3 = Me; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 R3 = Me; R6 = Ph; R5 = Me Et c-Pr 32 R3 = Me ; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 R3 = Me; R6 = Ph; R5 = CH2CO2Me OH OMe 34 R3 = Me ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 35 R3 = Me ; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 36 R3 = Me; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 R3 = OMe; R6 = Me; R5 = Me i-Pr c-Pr 38 R3 = OMe; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 R3 = OMe; R6 = Me; R5 = CH2CO2Me OH OMe 40 R3 = OMe; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 R3 = OMe; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 42 R3 = OMe; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 R3 = OMe; R6 = Ph; R5 = Me Et c-Pr 44 R3 = OMe; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 45 R3 = OMe; R6 = Ph; R5 = CH2CO2Me OH OMe 46 R3 = OMe; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 47 R3 = OMe; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 48 R3 = OMe; R6 = Ph; R5 = CONMe2 SO2CF3 P (O) (OMe) Me TABLE 8 (R2 = c-Pr) COLUMN 1 2 3 1 R3 = Cl; R6 = Me; R5 = Me i-Pr c-Pr 2 R3 = Cl; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 3 R3 = Cl ; R6 = Me; R5 = CH2CO2Me OH OMe 4 R3 = Cl ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 5 R3 = Cl ; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 6 R3 = Cl; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Cl;7R3 Ph;R5=MeEtc-Pr= 8 R3 = Cl ; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 9 R3 = Cl; R6 = Ph; R5 = CH2CO2Me OH OMe 10 R3 = Cl ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 11 R3 = Cl; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 12 R3 = Cl; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 13 R3 = Br; R6 = Me ; R5 = Me i-Pr c-Pr 14 R3 = Br; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 15 R3 = Br ; R6 = Me; R5 = CH2CO2Me OH OMe 16 R3 = Br ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 17 R3 = Br ; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 18 R3 = Br; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 19 R3 = Br; R6 = Ph ; R5 = Me Et c-Pr 20 R3 = Br ; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 21 R3 = Br; R6 = Ph; R5 = CH2CO2Me OH OMe 22 R3 = Br ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 23 R3 = Br ; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 24 R3 = Br; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 25 R3 = Me; R6 = Me; R5 = Me i-Pr c-Pr 26 R3 = Me; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 27 R3 = Me; R6 = Me; R5 = CH2CO2Me OH OMe 28 R3 = Me ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 R3 = Me; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 30 R3 = Me; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 R3 = Me; R6 = Ph; R5 = Me Et c-Pr 32 R3 = Me; R6 = Ph ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 R3 = Me ; R6 = Ph; R5 = CH2CO2Me OH OMe 34 R3 = Me; R6 = Ph ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 35 R3 = Me; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 36 R3 = Me; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 37 R3 = OMe; R6 = Me; R5 = Me i-Pr c-Pr 38 R3 = OMe; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 R3 = OMe; R6 = Me; R5 = CH2CO2Me OH OMe 40 R3 = OMe; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 R3 = OMe; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 42 R3 = OMe; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 R3 = OMe; R6 = Ph; R5 = Me Et c-Pr 44 R3 = OMe; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 45 R3 = OMe; R6 = Ph; R5 = CH2CO2Me OH OMe 46 R3 = OMe; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 47 R3 = OMe; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 48 R3 = OMe; R6 = Ph; R5 = CON Me2 SO2CF3 P (O) (OMe) Me TABLE 9 (X = 0) COLUMN 1 2 3 =Q-1;R6=Me;R5=Mei-Prc-Pr1G 2 G = Q-1; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-1;3G Me;R5=CH2CO2MeOHOMe= =Q-1;R6=Me;R5=OCH2CNO(CH2)2CF=CF2COMe4G 5 G = Q-1; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 6 G = Q-1; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 7 G = Q-1 ; R6 = Ph; R5 = Me Et c-Pr 8 G = Q-1; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 9 G = Q-1; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-1;R6=Ph;10G OCH2CNO(CH2)2CF=CF2COMe= =Q-1;R6=Ph;11G CO-t-BuCO2MeCO2-t-Bu= 12 G = Q-1; R6 = Ph ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 13 G = Q-2; R6 = Me ; R5 = Me i-Pr c-Pr 14 G = Q-2; R6 = Me ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-2;15G Me;R5=CH2CO2MeOHOMe= 16 G = Q-2; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 17 G = Q-2; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 18 G = Q-2; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-2;19G Ph;R5=MeEtc-Pr= =Q-2;20G Ph;R5=CH2CNCH2OMe(CH2)2CF=CF2= 21 G = Q-2; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-2;22G Ph;R5=OCH2CNO(CH2)2CF=CF2COMe= =Q-2;23G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 24 G = Q-2; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 25 G = Q-3 ; R6 = Me ; R5 = Me i-Pr c-Pr 26 G = Q-3; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 G = Q-3; R6 = Me ; R5 = CH2CO2Me OH OMe =Q-3;28G Me;= R5 O(CH2)2CF=CF2COMeOCH2CN 29 G = Q-3; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 30 G = Q-3; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-3; R6 = Ph; R5 = Me Et c-Pr 32 G = Q-3; R6 = Ph; R5= CH2CN CH20Me (CH2) 2CF=CF2 33 G = Q-3; R6 = Ph; R5 = CH2CO2Me OH OMe 34 G = Q-3; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-3;R6=Ph;R5=CO-t-BuCO2MeCO2-t-Bu35G 36 G = Q-3; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-4; R6 = Me; R5 = Me i-Pr c-Pr 38 G = Q-4; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-4; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-4; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-4; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 42 G = Q-4; R6 = Me; R5= CONMe2 S02CF3 P (O) (OMe) Me =Q-4;43G Ph;R5=MeEtc-Pt= 44 G = Q-4; R5=CH2CNCH20Me (CH2) 2CF=CF2 45 G = Q-4; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-4;46G Ph;R5=OCH2CNO(CH2)2CF=CF2COMe= =Q-4;47G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 48 G = Q-4; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me TABLE 10 COLUMN (X = S) 1 2 3 =Q-1;R6=Me;R5=Mei-Prc-Pr1G 2 G = Q-1 ; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 3 G = Q-1 ; R6 = Me; R5 = CH2CO2Me OH OMe 4 G = Q-1 ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 5 G = Q-1 ; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 6 G = Q-1 ; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 7 G = Q-1 ; R6 = Ph ; R5 = Me Et c-Pr =Q-1;R6=Ph;R5=CH2CNCH2OMe(CH2)2CF=CF28G =Q-1;R6=Ph;9G CH2CO2MeOHOMe= =Q-1;R6=Ph;10G OCH2CNO(CH2)2CF=CF2COMe= =Q-1;R6=Ph;11G CO-t-BuCO2MeCO2-t-Bu= 12 G = Q-1 ; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 13 G = Q-2 ; R6 = Me ; R5 = Me i-Pr c-Pr 14 G = Q-2; R6 = Me ; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 15 G = Q-2; R6 = Me ; R5 = CH2CO2Me OH OMe 16 G = Q-2; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-2;R6=Me;R5=CO-t-BuCO2MeCO2-t-Bu17G 18 G = Q-2; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 19 G = Q-2; R6 = Ph; R5 = Me Et c-Pr 20 G = Q-2; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 21 G = Q-2; R6 = Ph; R5 = CH2CO2Me OH OMe 22 G = Q-2; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =O-2;23G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 24 G = Q-2; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 25 G = Q-3; R6 = Me; R5 = Me i-Pr c-Pr 26 G = Q-3; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 G = Q-3; R6 = Me; R5 = CH2CO2Me OH OMe 28 G = Q-3; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 G = Q-3; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 30 G = Q-3; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-3; R6 = Ph; R5 = Me Et c-Pr 32 G = Q-3; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-3;33G Ph;R5=CH2CO2MeOHOMe= 34 G = Q-3; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-3;R6=Ph;R5=CO-t-BuCO2MeCO2-t-Bu35G 36 G = Q-3; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-4; R6 = Me ; R5 = Me i-Pr c-Pr 38 G = Q-4; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-4; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-4; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-4; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 42 G = Q-4; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 G = Q-4; R6 = Ph; R5 = Me Et c-Pr 44 G = Q-4; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-4;45G Ph;R5=CH2CO2MeOHOMe= =1-4;46G Ph;R5=OCH2CNO(CH2)2CF=CF2COMe= 47 G = Q-4 ; R6 = Ph ; R5 = CO-t-Bu C02Me C02-t-Bu 48 G = Q-4; R6 = Ph; R5 = CONMe2 SO2CF3 P (O) (OMe) Me TABLE 11 (X = NH) COLUMN 312 1 G = Q-5; R6 = Me; R5 = Me i-Pr c-Pr 2 G = Q-5; R6 = Me; R5 = t-Bu c-Hex Bn 3 G = Q-5; R6 = Me ; R5 = CH2CN CH20Me CH2SO2Me 4 G = Q-5; R6 = Me ; R5 = OH OMe (CH2) 2CF=CF2 5 G = Q-5; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 6 G = Q-5; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 7 G = Q-5; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 8 G = Q-5; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 9 G = Q-5; R6 = Ph; R5 = Me Et i-Pr =Q-5;R6=Ph;10G c-Prc-PenBn= 11 G = Q-5; R6 = Ph; R5 = CH2CN CH2OMe CH2SO2Me 12 G = Q-5; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 13 G = Q-5; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 14 G = Q-5; R6 = Ph; R5 = CO-t-Bu CH2CO2Me CO2Me 15 G = Q-5; R6 = Ph; R5C02-/-BuCONMe2S02Me 16 G = Q-5; R6 = Ph; R5 = SO2CF3 P(O) (OMe) 2 P (O) (OMe) Me 17 G = Q-6; R6 = Me; R5 = Me i-Pr c-Pr 18 G = Q-6; R6 = Me ; R5 = t-Bu c-Hex Bn 19 G = Q-6; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 20 G = Q-6; R6 = Me ; R5 = OH OMe (CH2) 2CF=CF2 21 G = Q-6; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 22 G = Q-6; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 23 G = Q-6; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 24 G = Q-6; R6 = Me ; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 25 G = Q-6; R6 = Ph; R5 = Me Et i-Pr 26 G = Q-6; R6 = Ph; R5 = c-Pr c-Pen Bn =Q-6;27G Ph;R5=CH2CNCH2OMeCH2SO2Me= 28 G = Q-6; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 29 G = Q-6; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 30 G = Q-6; R6 = Ph; R5 = CO-t-Bu CH2CO2Me CO2Me 31 G = Q-6; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 32 G = Q-6; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 33 G = Q-7; R6 = Me; R5 = Me i-Pr c-Pr 34 G = Q-7; R6 = Me; R5 = t-Bu c-Hex Bn 35 G = Q-7; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 36 G = Q-7; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 37 G = Q-7; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 38 G = Q-7 ; R6 = Me ; R5 = CO-t-Bu CH2CO2Me CO2Me 39 G = Q-7; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 40 G = Q-7; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me =Q-7;R6=Ph;41G MeEti-Pr= =Q-7;42G Ph;R5=c-Prc-PenBn= =Q-7;43G Ph;R5=CH2CNCH2OMeCH2SO2Me= 44 G = Q-7 ; R6 = Ph ; R5 = OH OMe (CH2) 2CF=CF2 45 G = Q-7; R6 = Ph ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-7;46G Ph;R5=CO-t-BuCH2CO2MeCO2Me= 47 G = Q-7; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 48 G = Q-7; R6 = Ph; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 49 G = Q-8; R6 = Me; R5 = Me i-Pr c-Pr 50 G = Q-8; R6 = Me; R5 = t-Bu c-Hex Bn 51 G = Q-8 ; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 52 G = Q-8; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 53 G = Q-8; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 54 G = Q-8; R6 = Me ; R5= CO-t-Bu CH2CO2Me C02Me 55 G = Q-8; R6 = Me ; R5 = C02-t-Bu CONMe2 S02Me 56 G = Q-8; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 57 G = Q-8; R6 = Ph; R5 = Me Et i-Pr =Q-8;58G Ph;R5=c-Prc-PenBn= =Q-8;59G Ph;R5=CH2CNCH2OMeCH2SO2Me= 60 G = Q-8; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 61 G = Q-8; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 62 G = Q-8; R6 = Ph; R5 = CO-t-Bu CH2CO2Me CO2Me =Q-8;63G Ph;R5=CO2-t-BuCONMe2SO2Me= 64 G = Q-8; R6 = Ph; R5 = SO2CF3 P(O) (OMe) 2 P (O) (OMe) Me 65 G = Q-9; R6 = Me; R5 = Me i-Pr c-Pr 66 G = Q-9; R6 = Me; R5 = t-Bu c-Hex Bn 67 G = Q-9; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 68 G = Q-9; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 69 G = Q-9; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 70 G = Q-9; R6 =CO-t-BuCH2C02MeC02Me 71 G = Q-9; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 72 G = Q-9; R6 = Me; R5 = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 73 G = Q-9; R6 = Ph; R5 = Me Et i-Pr 74 G = Q-9; R6 = Ph; R5 = c-Pr c-Pen Bn 75 G = Q-9; R6 = Ph; R5 = CH2CN CH20Me CH2S02Me 76 G = Q-9; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 77 G = Q-9; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-9;78G Ph;R5=CO-t-BuCH2CO2MeCO2Me= 79 G = Q-9; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 80 G = Q-9; R6 = Ph; RS = S02CF3 P (O) (OMe) 2 P (O) (OMe) Me 81 G = Q-10; R6 = Me; R5 = Me i-Pr c-Pr 82 G = Q-10; R6 = Me; R5 = t-Bu c-Hex Bn 83 G = Q-10 ; R6 = Me; R5 = CH2CN CH20Me CH2S02Me 84 G = Q-10; R6 = Me; R5 = OH OMe (CH2) 2CF=CF2 85 G = Q-10; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 86 G = Q-10 ; R6 = Me; R5 = CO-t-Bu CH2C02Me C02Me 87 G = Q-10; R6 = Me; R5 = C02-t-Bu CONMe2 S02Me 88 G = Q-10; R6 = Me; R5 = SO2CF3 P(O) (OMe) 2 P (O) (OMe) Me 89 G = Q-10; R6 = Ph; R5 = Me Et i-Pr 90 G = Q-10 ; R6 = Ph; R5 = c-Pr c-Pen Bn =Q-10;R6=Ph;91G CH2CNCH2OMeCH2SO2Me= 92 G = Q-10 ; R6 = Ph; R5 = OH OMe (CH2) 2CF=CF2 93 G = Q-10; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 94 G = Q-10 ; R6 = Ph; R5 = CO-t-Bu CH2C02Me C02Me 95 G = Q-10; R6 = Ph; R5 = C02-t-Bu CONMe2 S02Me 96 G = Q-10 ; R6 = Ph; R5 = SO2CF3 P(O) (OMe) 2 P (O) (OMe) Me TABLE 12 (X = O) COLUMN 1 2 3 1 G = Q-5 ; R6 = Me; R5 = Me i-Pr c-Pr 2 G = Q-5; R6 = Me ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 3 G = Q-5; R6 = Me; R5 = CH2CO2Me OH OMe 4 G = Q-5; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 5 G = Q-5; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 6 G = Q-5; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 7 G = Q-5 ; R6 = Ph ; R5 = Me Et c-Pr 8 G = Q-5; R5=CH2CNCH20Me (CH2) 2CF=CF2 9 G = Q-5; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-5;R6=Ph;R5=OCH2CNO(CH2)2CF=CF2COMe10G 11 G = Q-5; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 12 G = Q-5; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 13 G = Q-6; R6 = Me ; R5 = Me i-Pr c-Pr 14 G = Q-6; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 15 G = Q-6; R6 = Me; R5 = CH2CO2Me OH OMe 16 G = Q-6 ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 17 G = Q-6; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 18 G = Q-6; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-6;19G Ph;R5=MeEtc-Pr= 20 G = Q-6; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 21 G = Q-6; R6 = Ph; R5 = CH2CO2Me OH OMe 22 G = Q-6; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 23 G = Q-6; R6 = Ph ; R5 = CO-t-Bu C02Me C02-t-Bu 24 G = Q-6; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-7;25G Me;R5=Mei-Prc-Pr= 26 G = Q-7; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 27 G = Q-7; R6 = Me; R5 = CH2CO2Me OH OMe 28 G = Q-7; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 G = Q-7; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 30 G = Q-7; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-7; R6 = Ph; R5 = Me Et c-Pr 32 G = Q-7; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 G = Q-7; R6 = Ph; R5 = CH2CO2Me OH OMe 34 G = Q-7; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 35 G = Q-7; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 36 G = Q-7 ; R6 = Ph ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-8; R6 = Me; R5 = Me i-Pr c-Pr 38 G = Q-8; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-8; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-8; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-8; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 42 G = Q-8; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 G = Q-8 ; R6 = Ph ; R5 = Me Et c-Pr 44 G = Q-8; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 45 G = Q-8; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-8;46G Ph;R5=OCH2CNO(CH2)2CF=CF2COMe= =Q-8;R6=Ph;R5=CO-t-BuCO2MeCO2-t-Bu47G 48 G = Q-8; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 49 G = Q-9; R6 = Me ; R5 = Me i-Pr c-Pr 50 G = Q-9; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 51 G = Q-9; R6 = Me; R5 = CH2CO2Me OH OMe 52 G = Q-9; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 53 G = Q-9; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 54 G = Q-9; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 55 G = Q-9; R6 = Ph; R5 = Me Et c-Pr 56 G = Q-9; R6 = Ph ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-9;57G Ph;R5=CH2CO2MeOHOMe= 58 G = Q-9; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 59 G = Q-9; R6 = Ph ; R5 = CO-t-Bu C02Me C02-t-Bu 60 G = Q-9; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 61 G = Q-10; R6 = Me; R5 = Me i-Pr c-Pr 62 G = Q-10; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 63 G = Q-10; R6 = Me ; R5 = CH2CO2Me OH OMe 64 G = Q-10; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 65 G = Q-10; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 66 G = Q-10; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-10;R6=Ph;R5=MeEtc-Pr67G =Q-10;68G Ph;R5=CH2CNCH2OMe(CH2)2CF=CF2= 69 G = Q-10; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-10;R6=Ph;R5=OCH2CNO(CH2)2CF=CF2COMe70G =Q-10;R6=Ph;R5=CO-t-BuCO2MeCO2-t-Bu71G =Q-10;R6=Ph;R5=CONMe2SO2CF3P(O)(OMe)Me72G TABLE 13 (X = S) COLUMN 1 2 3 1 G = Q-5 ; R6 = Me; R5 = Me i-Pr c-Pr 2 G = Q-5; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-5;R6=Me;R5=CH2CO2MeOHOMe3G 4 G = Q-5; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 5 G = Q-5; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 6 G = Q-5; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 7 G = Q-5; R6 = Ph; R5 = Me Et c-Pr 8 G = Q-5; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 9 G = Q-5; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-5;R6=Ph;R5=OCH2CNO(CH2)2CF=CF2COMe10G 11 G = Q-5; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 12 G = Q-5; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 13 G = Q-6; R6 = Me; R5 = Me i-Pr c-Pr 14 G = Q-6; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 15 G = Q-6; R6 = Me; R5 = CH2CO2Me OH OMe 16 G = Q-6; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 17 G = Q-6; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 18 G = Q-6; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 19 G = Q-6; R6 = Ph; R5 = Me Et c-Pr 20 G = Q-6; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 21 G = Q-6; R6 = Ph; R5 = CH2CO2Me OH OMe 22 G = Q-6; R6 = Ph ; RS = OCH2CN O (CH2) 2CF=CF2 COMe 23 G = Q-6; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 24 G = Q-6; R6 = Ph ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 25 G = Q-7; R6 = Me; R5 = Me i-Pr c-Pr 26 G = Q-7; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 G = Q-7; R6 = Me; R5 = CH2CO2Me OH OMe 28 G = Q-7; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 G = Q-7; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 30 G = Q-7; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-7 ; R6 = Ph ; RS = Me Et c-Pr 32 G = Q-7; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 G = Q-7; R6 = Ph; R5 = CH2CO2Me OH OMe 34 G = Q-7; R6 = Ph ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-7;35G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 36 G = Q-7; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-8; R6 = Me; R5 = Me i-Pr c-Pr 38 G = Q-8; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-8; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-8; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-8; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 42 G = Q-8; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 G = Q-8 ; R6 = Ph; R5 = Me Et c-Pr 44 G = Q-8; R5=CH2CNCH20Me (CH2) 2CF=CF2 45 G = Q-8; R6 = Ph; R5 = CH2CO2Me OH OMe 46 G = Q-8; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-8;47G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 48 G = Q-8; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 49 G = Q-9; R6 = Me; R5 = Me i-Pr c-Pr 50 G = Q-9; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 51 G = Q-9; R6 = Me; R5 = CH2CO2Me OH OMe 52 G = Q-9; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 53 G = Q-9; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 54 G = Q-9; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-9;55G Ph;R5=MeEtc-Pr= 56 G = Q-9; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 57 G = Q-9 ; R6 = Ph ; RS = CH2C02Me OH OMe 58 G = Q-9; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 59 G = Q-9; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 60 G = Q-9; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 61 G = Q-10; R6 = Me; R5 = Me i-Pr c-Pr 62 G = Q-10; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 63 G = Q-10 ; R6 = Me; R5 = CH2CO2Me OH OMe 64 G = Q-10; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 65 G = Q-10; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 66 G = Q-10; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 67 G = Q-10 ; R6 = Ph; R5 = Me Et c-Pr 68 G = Q-10 ; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-10;R6=Ph;R5=CH2CO2MeOHOMe69G =Q-10;70G Ph;= OCH2CNO(CH2)2CF=CF2COMe= 71 G = Q-10; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 72 G = Q-10; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me TABLE 14 (X = NH) COLUMN 312 =Q-11;R6=Me;R5=Mei-Prc-Pr1G 2 G = Q-11 ; R6 = Me ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 3 G = Q-ll ; R6= Me; R5= CH2C02Me OH OMe 4 G = Q-ll ; R6= Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-11;R6=Me;5G CO-t-BuCO2MeCO2-t-Bu= 6 G = Q-ll; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-11;R6=Ph;7G MeEtc-Pr= =Q-11;R6=Ph;R5=CH2CNCH2OMe(CH2)2CF=CF28G =Q-11;R6=Ph;R5=CH2CO2MeOHOMe9G =Q-11;R6=Ph;10G OCH2CNO(CH2)2CF=CF2COMe= =Q-11;R6=Ph;11G CO-t-BuCO2MeCO2-t-Bu= 12 G = Q-ll ; R6= Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me =Q-12;13G Me;R5=Mei-Prc-Pr= 14 G = Q-12; R6 = Me ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-12;15G Me;R5=CH2CO2MeOHOMe= =Q-12;16G Me;R5=OCH2CNO(CH2)2CF=CF2COMe= 17 G = Q-12; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 18 G = Q-12; R6 = Me ; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-12;19G Ph;R5=MeEtc-Pr= 20 G = Q-12 ; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-12;21G Ph;R5=CH2CO2MeOHOMe= =Q-12;22G Ph;R5=OCH2CNO(CH2)2CF=CF2COMe= =Q-12;23G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 24 G = Q-12; R6 = Ph ; R5 = CONMe2 SO2CF3 P (O) (OMe) Me 25 G = Q-13; R6 = Me ; R5 = Me i-Pr c-Pr 26 G = Q-13; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 G = Q-13; R6 = Me; R5 = CH2CO2Me OH OMe 28 G = Q-13; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-13;R6=Me;R5=CO-t-BuCO2MeCO2-t-Bu29G 30 G = Q-13 ; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-13 ; R6 = Ph; R5 = Me Et c-Pr 32 G = Q-13; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 G = Q-13; R6 = Ph; R5 = CH2CO2Me OH OMe 34 G = Q-13 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 35 G = Q-13; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 36 G = Q-13; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-14; R6 = Me ; R5 = Me i-Pr c-Pr 38 G = Q-14; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-14; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-14; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-14; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 42 G = Q-14; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 G = Q-14; R6 = Ph; R5 = Me Et c-Pr 44 G = Q-14; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 45 G = Q-14 ; R6 = Ph; R5 = CH2CO2Me OH OMe 46 G = Q-14 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 47 G = Q-14 ; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 48 G = Q-14; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 49 G = Q-15; R6 = Me; R5 = Me i-Pr c-Pr 50 G = Q-15; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 51 G = Q-15; R6 = Me; R5 = CH2CO2Me OH OMe 52 G = Q-15; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 53 G = Q-15; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 54 G = Q-15; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 55 G = Q-15; R6 = Ph; R5 = Me Et c-Pr 56 G = Q-15; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 57 G = Q-15; R6 = Ph; R5 = CH2CO2Me OH OMe 58 G = Q-15; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 59 G = Q-15; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 60 G = Q-15; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 61 G = Q-16; R6 = Me; R5 = Me i-Pr c-Pr 62 G = Q-16; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 63 G = Q-16; R6 = Me; R5 = CH2CO2Me OH OMe 64 G = Q-16; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 65 G = Q-16; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 66 G = Q-16; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 67 G = Q-16; R6 = Ph; R5 = Me Et c-Pr 68 G = Q-16 ; R6 = Ph; RS = CH2CN CH20Me (CH2) 2CF=CF2 69 G = Q-16; R6 = Ph ; R5 = CH2CO2Me OH OMe 70 G = Q-16; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-16;71G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 72 G = Q-16; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 73 G = Q-17; R6 = Me; R5 = Me i-Pr c-Pr 74 G = Q-17; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 75 G = Q-17; R6 = Me; R5 = CH2CO2Me OH OMe 76 G = Q-17 ; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 77 G = Q-17; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 78 G = Q-17; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 79 G = Q-17; R6 = Ph; R5 = Me Et c-Pr 80 G = Q-17 ; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-17;R6=Ph;81G CH2CO2MeOHOMe= 82 G = Q-17 ; R6 = Ph; RS = OCH2CN O (CH2) 2CF=CF2 COMe 83 G = Q-17; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 84 G = Q-17; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me TABLE 15 (X = O) COLUMN 1 2 3 =Q-11;R6=Me;R5=Mei-Prc-Pr1G =Q-11;R6=Me;R5=CH2CNCH2OMe(CH2)2CF=CF22G =Q-11;R6=Me;R5=CH2CO2MeOHOMe3G =Q-11;R6=Me;R5=OCH2CNO(CH2)2CF=CF2COMe4G =Q-11;R6=Me;R5=CO-t-BuCO2MeCO2-t-Bu5G =Q-11;R6=Me;R5=CONMe2SO2CF3P(O)(OMe)Me6G =Q-11;R6=Ph;R5=MeEtc-Pr7G =Q-11;R6=Ph;R5=CH2CNCH2OMe(CH2)2CF=CF28G =Q-11;R6=Ph;R5=CH2CO2MeOHOMe9G =Q-11;R6=Ph;10G OCH2CNO(CH2)2CF=CF2COMe= =Q-11;R6=Ph;R5=CO-t-BuCO2MeCO2-t-Bu11G 12 G = Q-11 ; R6 = Ph ; RS = CONMe2 S02CF3 P (O) (OMe) Me =Q-12;R6=Me;13G Mei-Prc-Pr= 14 G = Q-12 ; R6 = Me ; R5= CH2CN CH20Me (CH2) 2CF=CF2 15 G = Q-12 ; R6 = Me; R5= CH2C02Me OH OMe =Q-12;R6=Me;R5=OCH2CNO(CH2)2CF=CF2COMe16G 17 G = Q-12 ; R6 = Me ; R5= CO-t-Bu C02Me C02-t-Bu =Q-12;R6=Me;R5=CONMe2SO2CF3P(O)(OMe)Me18G =Q-12;19G Ph;R5=MeEtc-Pr= 20 G = Q-12; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-12;21G Ph;R5=CH2CO2MeOHOMe= 22 G = Q-12; R6 = Rh; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 23 G = Q-12; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 24 G = Q-12; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 25 G = Q-13; R6 = Me; R5 = Me i-Pr c-Pr 26 G = Q-13; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 G = Q-13; R6 = Me ; R5 = CH2CO2Me OH OMe 28 G = Q-13 ; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 G = Q-13; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 30 G = Q-13 ; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-13; R6 = Ph; R5 = Me Et c-Pr 32 G = Q-13; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 33 G = Q-13; R6 = Ph; R5 = CH2CO2Me OH OMe 34 G = Q-13; R6 = Ph ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-13;35G Ph;R5=CO-t-BuCO2MeCO2-t-Bu= 36 G = Q-13 ; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-14; R6 = Me; R5 = Me i-Pr c-Pr 38 G = Q-14; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-14; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-14; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-14 ; R6 = Me ; RS = CO-t-Bu C02Me C02-t-Bu 42 G = Q-14; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 G = Q-14; R6 = Ph; R5 = Me Et c-Pr 44 G = Q-14; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 45 G = Q-14; R6 = Ph; R5 = CH2CO2Me OH OMe 46 G = Q-14 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 47 G = Q-14; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 48 G = Q-14; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 49 G = Q-15; R6 = Me; R5 = Me i-Pr c-Pr 50 G = Q-15; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 51 G = Q-15; R6 = Me; R5 = CH2CO2Me OH OMe 52 G = Q-15 ; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 53 G = Q-15; R6 = Me; R5= CO-t-Bu C02Me C02-t-Bu 54 G = Q-15 ; R6 = Me ; RS = CONMe2 S02CF3 P (O) (OMe) Me 55 G = Q-15; R6 = Ph; R5 = Me Et c-Pr 56 G = Q-15; R5=CH2CNCH20Me (CH2) 2CF=CF2 57 G = Q-15; R6 = Ph; R5 = CH2CO2Me OH OMe 58 G = Q-15; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 59 G = Q-15; R6 = Ph ; R5 = CO-t-Bu C02Me C02-t-Bu 60 G = Q-15; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-16;R6=Me;R5=Mei-Prc-Pr61G =Q-16;R6=Me;R5=CH2CNCH2OMe(CH2)2CF=CF262G =Q-16;R6=Me;R5=CH2CO2MeOHOMe63G =Q-16,R6=Me;R5=OCH2CNO(CH2)2CF=CF2COMe64G 65 G = Q-16 ; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 66 G = Q-16; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 67 G = Q-16; R6 = Ph; R5 = Me Et c-Pr 68 G = Q-16; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 69 G = Q-16; R6 = Ph; R5 = CH2CO2Me OH OMe 70 G = Q-16; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 71 G = Q-16; R6 = Ph; R5 = CO-t-Bu CO2Me CO2-t-Bu 72 G = Q-16; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 73 G = Q-17; R6 = Me ; R5 = Me i-Pr c-Pr 74 G = Q-17 ; R6 = Me ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 75 G = Q-17; R6 = Me; R5 = CH2CO2Me OH OMe =Q-17;R6=Me;R5=OCH2CNO(CH2)2CF=CF2COMe76G =Q-17;R6=Me;R5=CO-t-BuCO2MeCO2-t-Bu77G 78 G = Q-17; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 79 G = Q-17; R6 = Ph; R5 = Me Et c-Pr 80 G = Q-17; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 81 G = Q-17; R6 = Ph; R5 = CH2CO2Me OH OMe 82 G = Q-17 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 83 G = Q-17; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 84 G = Q-17; R6 = Ph; R5 = CONMe2 SO2CF3 P (O) (OMe) Me TABLE 16 (X = S) COLUMN 1 2 3 =Q-11;R6=Me;R5=Mei-Prc-Pr1G 2 G = Q-11 ; R6 = Me; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 3 G = Q-11 ; R6 = Me; R5= CH2C02Me OH OMe =Q-11;R6=Me;4G R5 O(CH2)2CF=CF2COMeOCH2CN =Q-11;R6=Me;5G CO-t-BuCO2MeCO2-t-Bu= 6 G = Q-11 ; R6 = Me; R5= CONMe2 S02CF3 P (O) (OMe) Me 7 G = Q-11 ; R6 = Ph; R5= Me Et c-Pr 8 G = Q-11 ; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 9 G = Q-11 ; R6 = Ph; R5= CH2CO2Me OH OMe 10 G = Q-11 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 11 G = Q-11 ; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 12 G = Q-11 ; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 13 G = Q-12; R6 = Me ; R5 = Me i-Pr c-Pr =Q-12;R6=Me;R5=CH2CNCH2OMe(CH2)2CF=CF214G 15 G = Q-12; R6 = Me; R5 = CH2CO2Me OH OMe 16 G = Q-12; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 17 G = Q-12; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 18 G = Q-12; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 19 G = Q-12; R6 = Ph; R5 = Me Et c-Pr 20 G = Q-12 ; R6 = Ph; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 21 G = Q-12; R6 = Ph; R5 = CH2CO2Me OH OMe 22 G = Q-12; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 23 G = Q-12; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 24 G = Q-12 ; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 25 G = Q-13; R6 = Me ; R5 = Me i-Pr c-Pr 26 G = Q-13; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 27 G = Q-13; R6 = Me; R5 = CH2CO2Me OH OMe 28 G = Q-13; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 29 G = Q-13; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 30 G = Q-13; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 31 G = Q-13; R6 = Ph; R5 = Me Et c-Pr 32 G = Q-13; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 G = Q-13; R6 = Ph; R5 = CH2CO2Me OH OMe 34 G = Q-13; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 35 G = Q-13; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 36 G = Q-13; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 37 G = Q-14; R6 = Me ; R5 = Me i-Pr c-Pr 38 G = Q-14; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 39 G = Q-14; R6 = Me; R5 = CH2CO2Me OH OMe 40 G = Q-14; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 41 G = Q-14; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 42 G = Q-14 ; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 43 G = Q-14; R6 = Ph; R5 = Me Et c-Pr 44 G = Q-14; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 45 G = Q-14; R6 = Ph; R5 = CH2CO2Me OH OMe 46 G = Q-14 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q=14;R6=Ph;R5=CO-t-BuCO2MeCO2-t-Bu47G 48 G = Q-14; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 49 G = Q-15; R6 = Me; R5 = Me i-Pr c-Pr =Q-15;R6=Me;R5=CH2CNCH2OMe(CH2)2CF=CF250G 51 G = Q-15; R6 = Me; R5 = CH2CO2Me OH OMe 52 G = Q-15; R6 = Me; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 53 G = Q-15; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu =Q-15;R6=Me;R5=CONMe2SO2CF3P(O)(OMe)Me54G 55 G = Q-15; R6 = Ph; R5 = Me Et c-Pr 56 G = Q-15; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 57 G = Q-15; R6 = Ph; R5 = CH2CO2Me OH OMe 58 G = Q-15; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 59 G = Q-15; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 60 G = Q-15; R6 = Ph; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 61 G = Q-16; R6 = Me; R5 = Me i-Pr c-Pr 62G =Q-16= Me ; R5 =CH2CNCH20Me (CH2) 2CF=CF2 63 G = Q-16; R6 = Me; R5 = CH2CO2Me OH OMe 64 G = Q-16; R6 = Me ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 65 G = Q-16; R6 = Me; R5 = CO-t-Bu C02Me C02-t-Bu 66 G = Q-16; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 67 G = Q-16; R6 = Ph; R5 = Me Et c-Pr 68 G = Q-16; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 69 G = Q-16; R6 = Ph; R5 = CH2CO2Me OH OMe =Q-16;70G Ph;R5=OCH2CNO(CH2)2CF=CF2COMe= 71 G = Q-16; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 72 G = Q-16; R6 = Ph; R5 = CONMe2 S02CF3 P (O) (OMe) Me 73 G = Q-17; R6 = Me ; R5 = Me i-Pr c-Pr 74 G = Q-17; R6 = Me; R5 = CH2CN CH20Me (CH2) 2CF=CF2 75 G = Q-17; R6 = Me; R5 = CH2CO2Me OH OMe =Q-17;R6=Me;R5=OCH2CNO(CH2)2CF=CF2COMe76G 77 G = Q-17; R6 = Me ; R5 = CO-t-Bu C02Me C02-t-Bu 78 G = Q-17; R6 = Me; R5 = CONMe2 S02CF3 P (O) (OMe) Me 79 G = Q-17 ; R6 = Ph; R5 = Me Et c-Pr 80 G = Q-17; R6 = Ph; R5 = CH2CN CH20Me (CH2) 2CF=CF2 81 G = Q-17; R6 = Ph; R5 = CH2CO2Me OH OMe 82 G = Q-17 ; R6 = Ph; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 83 G = Q-17; R6 = Ph; R5 = CO-t-Bu C02Me C02-t-Bu 84 G = Q-17 ; R6 = Ph; R5 = CONMe2 SO2CF3 P (O) (OMe) Me TABLE 17 COLUMN 312 =Q-1;R5=HMeEt1G =Q-1;2G n-Prc-Prn-Bu= =Q-1;3G i-Bun-HexBn= =Q-1;4G CH2CH=CH2CH2CCl=CH2(CH2)2CF=CF2= =Q-1;5G CH2C#CHCH2-c-PrCH2CN= =Q-1;6G CH2CONH2CH2CONHMECH2CONMe2= 7 G = Q-1; R5 = CH20Me CH20Bn CH2SMe 8 G = Q-1; R5 = CH2S(O)Me CH2SO2Me (CH2) 20H 9 G = Q-1; R5 = (CH2) 20Me OH OMe =Q-1;10G OEtOCH2C#CHOCH2-c-Pr= =Q-1;11G OCH2CNO(CH2)2CF=CF2CHO= =Q-1;12G COMeCOEtCOCF3= =Q-1;13G CO-i-PrCO-c-PrCO-t-Bu= =Q-1;14G COPhCH2CO2MeCO2Me= 15 G = Q-1; R5 = C02Et C02-i-Pr C02-t-Bu =Q-1;16G CO2BnCONHMeCONMe2= 17 G = Q-1; R5 = S02Me S02CF3 S02Ph 18 G = Q-1; R5 = P (O) (OMe) 2 P (O) (OMe) Me Ph 19 G = Q-2; R5 = H Me Et 20 G = Q-2; R5 = n-Pr c-Pr n-Bu =Q-2;21G i-Bun-HexBn= 22 G = Q-2; R5 = CH2CH=CH2 CH2CCl=CH2 (CH2) 2CF=CF2 =Q-2;23G CH2C#CHCH2-c-PrCH2CN= 24 G = Q-2; R5 = CH2CONH2 CH2CONHMe CH2CONMe2 25 G = Q-2; R5 = CH20Me CH20Bn CH2SMe 26 G = Q-2; R5 = CH2S(O)Me CH2SO2Me (CH2) 20H 27 G = Q-2; R5 = (CH2) 20Me OH OMe =Q-2;28G OEtOCH2C#CHOCH2-c-Pr= 29 G = Q-2; R5 = OCH2CN O (CH2) 2CF=CF2 CHO =Q-2;30G COMeCOEtCOCF3= 31 G = Q-2; R5 = CO-i-Pr CO-c-Pr CO-t-Bu =Q-2;32G COPhCH2CO2MeCO2Me= 33 G = Q-2; R5 = C02Et C02-i-Pr C02-t-Bu =Q-2;34G CO2BnCONHMeCONMe2= 35 G = Q-2; R5 = S02Me S02CF3 S02Ph 36 G = Q-2; R5 = P(O) (OMe) 2 P (O) (OMe) Me Ph =Q-2;37G HMeEt= =Q-3;38G n-Prc-Prn-Bu= =Q-3;39G i-Bun-HexBn= 40 G = Q-3; R5 = CH2CH=CH2 CH2CCl=CH2 (CH2) 2CF=CF2 =Q-3;41G CH2C#CHCH2-c-PrCH2CN= 42 G = Q-3; R5 = CH2CONH2 CH2CONHMe CH2CONMe2 43 G = Q-3; R5 = CH20Me CH20Bn CH2SMe 44 G = Q-3; R5 = CH2S(O)Me CH2SO2Me (CH2) 20H 45 G = Q-3; R5 = (CH2)2OMe OH OMe =Q-3;46G OEtOCH2C#CHOCH2-c-Pr= 47 G = Q-3; R5 = OCH2CN O (CH2) 2CF=CF2 CHO =Q-3;48G COMeCOEtCOCF3= 49 G = Q-3; R5 = CO-i-Pr CO-c-Pr CO-t-Bu =Q-3;50G COPhCH2CO2MeCO2Me= =Q-3;51G CO2EtCO2-i-PrCO2-t-Bu= =Q-3;52G CO2BnCONHMeCONMe2= 53 G = Q-3; R5 = S02Me S02CF3 S02Ph 54 G = Q-3; R5 = P(O)(OMe)2 P(O) (OMe) Me Ph 55 G = Q-4; R5 = H Me Et 5656G=Q-4; n-Prc-Prn-Bu= 57 G = Q-4; R5 = i-Bu n-Hex Bn =Q-4;58G CH2CH=CH2CH2CCl=CH2(CH2)2CF=CF2= =Q-4;59G CH2C#CHCH2-c-PrCH2CN= =Q-4;60G CH2CONH2CH2CONHMeCH2CONMe2= 61 G = Q-4; R5 = CH20Me CH20Bn CH2SMe 62 G = Q-4; R5 = CH2S(O)Me CH2SO2Me (CH2) 20H 63 G = Q-4; R5 = (CH2) 20Me OH OMe =Q-4;64G OEtOCH2C#CHOCH2-c-Pr= 65 G = Q-4; R5 = OCH2CN O (CH2) 2CF=CF2 CHO =Q-4;66G COMeCOEtCOCF3= 67 G = Q-4; R5 = CO-i-Pr CO-c-Pr CO-t-Bu =Q-4;68G COPhCH2CO2MeCO2Me= 69 G = Q-4; R5 = C02Et C02-i-Pr C02-t-Bu =Q-4;70G CO2BnCONHMeCONMe2= 71 G = Q-4; R5 = S02Me S02CF3 S02Ph 72 G = Q-4; R5 = P(O)(OMe)2 P(O) (OMe) Me Ph TABLE 18 COLUMN 1 2 3 =Q-5;1G HMec-Pr= =Q-5;R5=CH2CNCH2OMe(CH2)2CF=CF22G =Q-5;3G CH2CO2MeOHOMe= =Q-5;4G OCH2CNO(CH2)2CF=CF2COMe= 5 G = Q-5; R5 = CO-t-Bu C02Me C02-t-Bu 6 G = Q-5; R5 = CONMe2 SO2CF3 P(O) (OMe) Me =Q-6;7G HMec-Pr= 8 G = Q-6; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-6;9G CH2CO2MeOHOMe= =Q-6;10G OCH2CNO(CH2)2CF=CF2COMe= 11 G = Q-6; R5 = CO-t-Bu C02Me C02-t-Bu 12 G = Q-6; R5 = CONMe2 SO2CF3 P(O) (OMe) Me =Q-7;13G HMec-Pr= 14 G = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-7;15G CH2CO2MeOHOMe= =Q-7;16G OCH2CNO(CH2)2CF=CF2COMe= =Q-7;17G CO-t-BuCO2MeCO2-t-Bu= 18 G = Q-7; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-8;19G HMec-Pr= 20 G = Q-8; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-8;21G CH2CO2MeOHOMe= =Q-8;22G OCH2CNO(CH2)2CF=CF2COMe= 23 G = Q-8; RS = CO-t-Bu C02Me C02-t-Bu 24 G = Q-8; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-9;25G HMec-Pr= 26 G = Q-9; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-9;27G CH2CO2MeOHOMe= =Q-9;28G OCH2CNO(CH2)2CF=CF2COMe= =Q-9;29G CO-t-BuCO2MeCO2-t-Bu= 30 G = Q-9; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-10;31G HMec-Pr= 32 G = Q-10; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-10;33G CH2CO2MeOHOMe= =Q-10;34G OCH2CNO(CH2)2CF=CF2COMe= =Q-10;35G CO-t-BuCO2MeCO2-t-Bu= 36 G = Q-10; R5 = CONMe2 SO2CF3 P(O) (OMe) Me =Q-11;37G R5 Mec-PrH 38 G = Q-11 ; R5= CH2CN CH20Me (CH2) 2CF=CF2 =Q-11;R5=CH2CO2MeOMeCOMe39G 40 G = Q-11 ; R5 = C02Me S02CF3 P (O) (OMe) Me =Q-12;41G HMec-Pr= 42 G = Q-12; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-12;43G CH2CO2MeOMeCOMe= 44 G = Q-12; R5 = C02Me S02CF3 P (O) (OMe) Me 45 G = Q-13; R5 = H Me c-Pr 46 G = Q-13; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-13;47G CH2CO2MeOMeCOMe= 48 G = Q-13; R5 = CO2Me SO2CF3 P (O) (OMe) Me 49 G = Q-14; R5 = H Me c-Pr 50 G = Q-14; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-14;51G CH2CH2MeOMeCOMe= 52 G = Q-14; R5 = CO2Me SO2CF3 P(O) (OMe) Me =Q-15;53G HMec-Pr= 54 G = Q-15; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-15;55G CH2CO2MeOHOMe= 56 G = Q-15; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 57 G = Q-15; R5 = CO-t-Bu C02Me C02-t-Bu 58 G = Q-15; R5 = CONMe2 S02CF3 P (O) (OMe) Me =Q-16;59G HMec-Pr= 60 G = Q-16; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-16;61G CH2CO2MeOMeCOMe= 62 G = Q-16; R5 = C02Me S02CF3 P (O) (OMe) Me 63 G = Q-17; R5 = H Me c-Pr 64 G = Q-17; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 =Q-17;65G CH2CO2MeOMeCOMe= 66 G = Q-17; R5 = CO2Me SO2CF3 P(O) (OMe) Me TABLE 19 COLUMN 1 2 3 1 G = Q-1 ; R6 = Q-2 ; R5 = H Me c-Pr 2 G = Q-1; R6 = Q-2; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 3 G = Q-1; R6 = Q-2; R5 = CH2CO2Me OH OMe =Q-1;4G Q-2;= OCH2CNO(CH2)2CF=CF2COMe= =Q-1;R6=Q-2;R5=CO-t-BuCO2MeCO2-t-Bu5G 6 G = Q-1; R6 = Q-2; R5 = CONMe2 SO2CF3 P(O)(OMe) Me 7 G = Q-1; R6 = Q-3; R5 = H Me c-Pr =Q-1;R6=Q-3;R5=CH2CNCH2OMe(CH2)2CF=CF28G 9 G = Q-1 ; R6 = Q-3; R5 = CH2CO2Me OH OMe 10 G = Q-1 ; R6 = Q-3; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 11 G = Q-1; R6 = Q-3; R5 = CO-t-Bu C02Me C02-t-Bu 12 G = Q-1; R6 = Q-3; R5 = CONMe2 S02CF3 P (O) (OMe) Me 13 G = Q-1 ; R6 = Q-4 ; R5 = H Me c-Pr 14 G = Q-1 ; R6 = Q-4; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 15 G = Q-1; R6 = Q-4; R5 = CH2CO2Me OH OMe 16 G = Q-1 ; R6 = Q-4 ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe =Q-1;R6=Q-4;R5=CO-t-BuCO2MeCO2-t-Bu17G =Q-1;R6=Q-4;R5=CONMe2SO2CF3P(O)(OMe)Me18G 19 G = Q-1; R6=Q-5; R5= H Me c-Pr 20 G = Q-1 ; R6 = Q-5; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 21 G = Q-1; R6 = Q-5; R5 = CH2CO2Me OMe COMe 22 G = Q-1 ; R6 = Q-5; R5 = C02Me S02CF3 P (O) (OMe) Me 23 G = Q-1; R6 = Q-6; R5 = H Me c-Pr =Q-1;R6=Q-6;R5=CH2CNCH2OMe(CH2)2CF=CF224G 25 G = Q-1; R6 = Q-6; R5 = CH2CO2Me OMe COMe =Q-1;R6=Q-6;R5=CO2MeSO2CF3P(O)(OMe)Me26G 27 G = Q-1 ; R6 = Q-7 ; R5 = H Me c-Pr 28 G = Q-1; R6 = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 29 G = Q-1; R6 = Q-7; R5 = CH2CO2Me OMe COMe 30 G = Q-1; R6 = Q-7; R5 = CO2Me SO2CF3 P(O) (OMe) Me 31 G = Q-1; R6=Q-8; R5 = H Me c-Pr 32 G = Q-1 ; R6 = Q-8; R5 = CH2CN CH20Me (CH2) 2CF=CF2 33 G = Q-1; R6 = Q-8; R5 = CH2CO2ME OMe COMe 34 G = Q-1; R6 = Q-8; R5 = C02Me S02CF3 P (O) (OMe) Me =Q-1;R6=Q-9;R5=HMec-Pr35G 36 G = Q-1; R6 = Q-9; R5 = CH2CN CH20Me (CH2) 2CF=CF2 =Q-1;R5=Q-9;R5=CH2CO2MeOMeCOMe37G =Q-1;R6=Q-9;R5=CO2MeSO2CF3P(O)(OMe)Me38G 39 G = Q-1; R6=Q-10; R5= H Me c-Pr =Q-1;R6=Q-10;R5=CH2CNCH2OMe(CH2)2CF=CF240G 41 G = Q-1; R6 = Q-10; R5 = CH2CO2Me OMe COMe 42 G = Q-1; R6 = Q-10; R5 = CO2Me SOWCF3 P (O) (OMe) Me 43 G = Q-1; R6 = Q-15; R5 = H Me c-Pr =Q-1;R6=Q-15;R5=CH2CNCH2OMe(CH2)2CF=CF244G 45 G = Q-1; R6 = Q-15; R5 = CH2CO2Me OMe COMe 46 G = Q-1 ; R6 = Q-15; R5 = C02Me S02CF3 P (O) (OMe) Me 47 G = Q-1; R6 = Q-16; R5 = H Me c-Pr =Q-1;R6=Q-16;R5=CH2CNCH2OMe(CH2)2CF=CF248G 49 G = Q-1 ; R6 = Q-16; R5 = CH2CO2Me OMe COMe 50 G = Q-1; R6 = Q-16; R5 = CO2Me SO2CF3 P(O) (OMe) Me 51 G = Q-1; R6 = Q-17; R5 = H Me c-Pr 52 G = Q-1; R6 = Q-17; R5 = CH2CN CH20Me (CH2) 2CF=CF2 53 G = Q-1 ; R6 = Q-17 ; R5 = CH2CO2Me OMe COMe =Q-1;R6=Q-17;R5=CO2MeSO2CF3P(O)(OMe)Me54G 55 G = Q-2; R6 = Q-1; R5 = Me Et c-Pr 56 G = Q-2; R6 = Q-1; R5 = CH2CN CH20Me (CH2) 2CF=CF2 57 G = Q-2 ; R6 = Q-1 ; R5 = CH2CO2Me OH OMe 58 G = Q-2; R6 = Q-1; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 59 G = Q-2; R6 = Q-1; R5 = CO-t-Bu C02Me C02-t-Bu 60 G = Q-2; R6 = Q-1; R5 = CONMe2 SO2CF3 P(O) (OMe) Me 61 G = Q-2; R6 = Q-3; R5 = H Me c-Pr 62 G = Q-2; R6 = Q-3; R5 = CH2CN CH20Me (CH2) 2CF=CF2 63 G = Q-2; R6 = Q-3; R5 = CH2CO2Me OH OMe 64 G = Q-2; R6 = Q-3; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 65 G = Q-2; R6 = Q-3; R5 = CO-t-Bu C02Me C02-t-Bu 66 G = Q-2; R6 = Q-3; R5 = CONMe2 S02CF3 P (O) (OMe) Me 67 G = Q-2; R6 = Q-4; R5 = H Me c-Pr 68 G = Q-2; R6 = Q-4; R5 = CH2CN CH20Me (CH2) 2CF=CF2 69 G = Q-2; R6 = Q-4; R5 = CH2CO2Me OH OMe 70 G = Q-2; R6 = Q-4; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 71 G = Q-2; R6 = Q-4; R5 = CO-t-Bu C02Me C02-t-Bu 72 G = Q-2; R6 = Q-4; R5 = CONMe2 S02CF3 P (O) (OMe) Me 73 G = Q-2; R6 = Q-5; R5 = H Me c-Pr 74 G = Q-2; R6 = Q-5; R5 = CH2CN CH20Me (CH2) 2CF=CF2 75 G = Q-2; R6 = Q-5; R5 = CH2CO2Me OMe COMe 76 G = Q-2; R6 = Q-5; R5 = C02Me S02CF3 P (O) (OMe) Me 77 G = Q-2; R6 = Q-6; R5= H Me c-Pr 78 G = Q-2; R6 = Q-6; R5 = CH2CN CH20Me (CH2) 2CF=CF2 79 G = Q-2; R6 = Q-6; R5 = CH2CO2Me OMe COMe 80 G = Q-2; R6 = Q-6; R5 = C02Me S02CF3 P (O) (OMe) Me 81 G = Q-2; R6 = Q-7; R5 = H Me c-Pr 82 G = Q-2; R6 = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 83 G = Q-2; R6 = Q-7; R5 = CH2CO2Me OMe COMe 84 G = Q-2; R6 = Q-7; R5 = C02Me S02CF3 P (O) (OMe) Me 85 G = Q-2; R6 = Q-8; R5 = H Me c-Pr 86 G = Q-2; R6 = Q-8; R5 = CH2CN CH20Me (CH2) 2CF=CF2 87 G = Q-2; R6 = Q-8; R5 = CH2CO2Me OMe COMe 88 G = Q-2; R6 = Q-8; R5 = C02Me S02CF3 P (O) (OMe) Me 89 G = Q-2; R6 = Q-9; R5 = H Me c-Pr 90 G = Q-2; R6 = Q-9; R5 = CH2CN CH20Me (CH2) 2CF=CF2 91 G = Q-2; R6 = Q-9; R5 = CH2CO2Me OMe COMe 92 G = Q-2; R6 = Q-9; R5 = CO2Me SO2CF3 P(O)(OMe)Me 93 G = Q-2; R6 = Q-10; R5 = H Me c-Pr 94 G = Q-2 ; R6 = Q-10 ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 95 G = Q-2 ; R6 = Q-10 ; R5 = CH2CO2Me OMe COMe 96 G = Q-2 ; R6 = Q-10 ; R5 = C02Me S02CF3 P (O) (OMe) Me 97 G = Q-2; R6 = Q-15 ; R5 = H Me c-Pr 98 G = Q-2; R6 = Q-15; R5 = CH2CN CH20Me (CH2) 2CF=CF2 99 G = Q-2; R6 = Q-15 ; RS = CH2C02Me OMe COMe 100 G = Q-2; R6 = Q-15; R5 = C02Me S02CF3 P (O) (OMe) Me 101 G = Q-3; R6 = Q-1; R5 = Me Et c-Pr 102 G = Q-3 ; R6 = Q-1 ; R5 = CH2CN CH20Me (CH2) 2CF=CF2 103 G = Q-3; R6 = Q-1; R5 = CH2CO2Me OH OMe 104 G = Q-3 ; R6 = Q-1 ; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 105 G = Q-3; R6 = Q-1; RS = CO-t-Bu C02Me C02-t-Bu 106 G = Q-3; R6 = Q-1; R5 = CONMe2 S02CF3 P (O) (OMe) Me 107 G = Q-3; R6 = Q-2; R5 = Me Et c-Pr 108 G = Q-3; R6 = Q-2; R5 = CH2CN CH20Me (CH2) 2CF=CF2 109 G = Q-3; R6 = Q-2; R5 = CH2CO2Me OH OMe 110 G = Q-3; R6 = Q-2; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 111 G = Q-3; R6 = Q-2; R5 = CO-t-Bu CO2Me CO2-t-Bu 112 G = Q-3; R6 = Q-2; R5 = CONMe2 S02CF3 P (O) (OMe) Me 113 G = Q-3; R6 = Q-4; R5 = H Me c-Pr 114 G = Q-3; R6 = Q-4; R5 = CH2CN CH20Me (CH2) 2CF=CF2 115 G = Q-3; R6 = Q-4; R5 = CH2CO2Me OH OMe 116 G = Q-3; R6 = Q4; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 117 G = Q-3; R6 = Q-4; R5 = CO-t-Bu C02Me C02-t-Bu 118 G = Q-3; R6 = Q-4; R5 = CONMe2 S02CF3 P (O) (OMe) Me 119 G = Q-3; R6 = Q-7; R5 = H Me c-Pr 120 G = Q-3; R6 = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 121 G = Q-3; R6 = Q-7; R5 = CH2CO2Me OMe COMe 122 G = Q-3; R6 = Q-7; R5 = C02Me S02CF3 P (O) (OMe) Me 123 G = Q-3; R6 = Q-8; R5 = H Me c-Pr 124 G = Q-3; R6 = Q-8; R5 = CH2CN CH20Me (CH2) 2CF=CF2 125 G = Q-3; R6 = Q-8; R5 = CH2CO2Me OMe COMe 126 G = Q-3; R6 = Q-8; R5 = C02Me S02CF3 P (O) (OMe) Me 127 G = Q-3; R6 = Q-9; R5 = H Me c-Pr 128 G = Q-3; R6 = Q-9; R5 = CH2CN CH20Me (CH2) 2CF=CF2 129 G = Q-3; R6 = Q-9; R5 = CH2CO2Me OMe COMe 130 G = Q-3; R6 = Q-9; R5 = C02Me S02CF3 P (O) (OMe) Me ! i 131 G = Q-3; R6 = Q-10; R5 = H Me c-Pr 132 G = Q-3; R6 = Q-10; R5 = CH2CN CH20Me (CH2) 2CF=CF2 133 G = Q-3; R6 = Q-10; R5 = CH2CO2Me OMe COMe 134 G = Q-3; R6 = Q-10; R5 = C02Me S02CF3 P (O) (OMe) Me 135 G = Q-3; R6 = Q-15; R5 = H Me c-Pr 136 G = Q-3 ; R6 = Q-15; R5 = CH2CN CH20Me (CH2) 2CF=CF2 137 G = Q-3; R6 = Q-15; R5 = CH2CO2Me OMe COMe 138 G = Q-3; R6 = Q-15; R5 = C02Me S02CF3 P (O) (OMe) Me 139 G = Q-4; R6 = Q-3; R5 = Me Et c-Pr 140 G = Q-4; R6 = Q-3; R5 = CH2CN CH20Me (CH2) 2CF=CF2 141 G = Q-4; R6 = Q-3; R5 = CH2CO2Me OH OMe 142 G = Q-4; R6 = Q-3; R5 = OCH2CN O (CH2) 2CF=CF2 COMe 143 G = Q-4; R6 = Q-3; R5 = CO-t-Bu C02Me C02-t-Bu 144 G = Q-4; R6 = Q-3; R5 = CONMe2 S02CF3 P (O) (OMe) Me 145 G = Q-4; R6 = Q-7; R5 = H Me c-Pr 146 G = Q-4; R6 = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 147 G = Q-4; R6 = Q-7; R5 = CH2CO2Me OMe COMe 148 G = Q-4; R6 = Q-7 ; R5 = C02Me S02CF3 P (O) (OMe) Me 149 G = Q-4; R6 = Q-8; R5 = H Me c-Pr 150 G = Q-4; R6 = Q-8; R5 = CH2CN CH20Me (CH2) 2CF=CF2 151 G = Q-4; R6 = Q-8; R5 = CH2CO2Me OMe COMe 152 G = Q-4; R6 = Q-8; R5 = C02Me S02CF3 P (O) (OMe) Me 153 G = Q-4; R6 = Q-9; R5 = H Me c-Pr 154 G = Q-4; R6 = Q-9; R5 = CH2CN CH20Me (CH2) 2CF=CF2 155 G = Q-4; R6 = Q-9; R5 = CH2C02Me OMe COMe 156 G = Q-4; R6 = Q-9; R5 = C02Me S02CF3 P (O) (OMe) Me 157 G = Q-4; R6 = Q-10; R5 = H Me c-Pr 158 G = Q-4; R6 = Q-10; R5 = CH2CN CH20Me (CH2) 2CF=CF2 159 G = Q-4; R6 = Q-10; R5 = CH2CO2Me OMe COMe 160 G = Q-4; R6 = Q-10; R5 = C02Me S02CF3 P (O) (OMe) Me 161 G = Q-4; R6 = Q-15; R5 = H Me c-Pr 162 G = Q-4; R6 = Q-15; R5 = CH2CN CH20Me (CH2) 2CF=CF2 163 G = Q-4; R6 = Q-15; R5 = CH2C02Me OMe COMe 164 G = Q-4; R6 = Q-15; R5 = C02Me S02CF3 P (O) (OMe) Me 165 G = Q-6; R6 = Q-7; R5 = H Me c-Pr 166 G = Q-6; R6 = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 167 G = Q-6; R6 = Q-7; R5 = CH2C02Me OMe COMe 168 G = Q-6; R6 = Q-7; R5 = C02Me S02CF3 P (O) (OMe) Me 169 G = Q-6; R6 = Q-8; R5 = H Me c-Pr 170 G = Q-6; R6 = Q-8; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 171 G = Q-6; R6 = Q-8; R5 = CH2CO2Me OMe COMe 172 G = Q-6; R6 = Q-8; R5 = C02Me S02CF3 P (O) (OMe) Me 173 G = Q-6; R6 = Q-9; R5 = H Me c-Pr 174 G = Q-6; R6 = Q-9; R5 = CH2CN CH20Me (CH2) 2CF=CF2 175 G = Q-6; R6 = Q-9; R5 = CH2CO2Me OMe COMe 176 G = Q-6; R6 = Q-9; R5 = CO2Me SO2CF3 P(O) (OMe) Me 177 G = Q-6; R6 = Q-10; R5 = H Me c-Pr 178 G = Q-6; R6 = Q-10; R5 = CH2CN CH2OMe (CH2) 2CF=CF2 179 G = Q-6; R6 = Q-10; R5 = CH2CO2Me OMe COMe 180 G = Q-6; R6 = Q-10; R5 = C02Me S02CF3 P (O) (OMe) Me 181 G = Q-6; R6 = Q-15 ; R5 = H Me c-Pr 182 G = Q-6; R6 = Q-15; R5 = CH2CN CH20Me (CH2) 2CF=CF2 183 G = Q-6; R6 = Q-15; R5 = CH2CO2Me OMe COMe 184 G = Q-6; R6 = Q-15; R5 = C02Me S02CF3 P (O) (OMe) Me 185 G = Q-9; R6 = Q-7; R5 = H Me c-Pr 186 G = Q-9 ; R6 = Q-7; R5 = CH2CN CH20Me (CH2) 2CF=CF2 187 G = Q-9; R6 = Q-7; R5 = CH2CO2Me OMe COMe 188 G = Q-9; R6 = Q-7; R5= C02Me S02CF3 P (O) (OMe) Me 189 G = Q-9; R6 = Q-8; R5 = H Me c-Pr 190 G = Q-9; R6 = Q-8; R5 = CH2CN CH20Me (CH2) 2CF=CF2 191 G = Q-9; R6 = Q-8; R5 = CH2CO2Me OMe COMe 192 G = Q-9; R6 = Q-8; R5 = C02Me S02CF3 P (O) (OMe) Me 193 G = Q-9; R6 = Q-10; R5 = H Me c-Pr 194 G = Q-9; R6 = Q-10; R5 = CH2CN CH20Me (CH2) 2CF=CF2 195 G = Q-9; R6 = Q-10; R5 = CH2CO2Me OMe COMe 196 G = Q-9; R6 = Q-10; R5 = C02Me S02CF3 P (O) (OMe) Me 197 G = Q-9; R6 = Q-15; R5 = H Me c-Pr 198 G = Q-9; R6 = Q-15; R5 = CH2CN CH20Me (CH2) 2CF=CF2 199 G = Q-9; R6 = Q-15; R5 = CH2CO2Me OMe COMe 200 G = Q-9; R6 = Q-15; R5 = CO2Me SO2CF3 P (O) (OMe) Me TABLE 20 COLUMN 1 2 3 4 1 G = Q-1; X = NH; NR5R6 = Piper Morph Phth Hphth 2 G = Q-2; X = NH; NR5R6 = Piper Morph Phth Hphth 3 G = Q-3; X = NH; NR5R6 = Piper Morph Phth Hphth 4 G = Q-4; X = NH; NR5R6 = Piper Morph Phth Hphth 5 G = Q-5; X = NH; NR5R6 = Piper Morph Phth Hphth 6 G = Q-6; X = NH; NR5R6 = Piper Morph Phth Hphth =Q-7;7G NH;NR5R6=PiperMorphPhthHphth= 8 G = Q-9; X = NH; NR5R6 = Piper Morph Phth Hphth 9 G = Q-10; X = NH ; NR5R6 = Piper Morph Phth Hphth 10 G = Q-15; X = NH; NR5R6 = Piper Morph Phth Hphth =Q-16;11G NH;NR5R6=PiperMorphPhthHphth= 12 G = Q-17; X = NH; NR5R6 = Piper Morph Phth Hphth 13 G = Q-1; X = O; NR5R6 = Piper Morph Phth Hphth 14 G = Q-2; X = O; NR5R6 = Piper Morph Phth Hphth 15 G = Q-3; X = O; NR5R6 = Piper Morph Phth Hphth 16 G = Q-4; X = O; NR5R6 = Piper Morph Phth Hphth 17 G = Q-5; X = O; NR5R6 = Piper Morph Phth Hphth 18 G = Q-6; X = O; NR5R6 = Piper Morph Phth Hphth 19 G = Q-7; X = O; NR5R6 = Piper Morph Phth Hphth 20 G = Q-9; X = O; NR5R6 = Piper Morph Phth Hphth 21 G = Q-10; X = O; NR5R6 = Piper Morph Phth Hphth 22 G = Q-15; X = O; NR5R6 = Piper Morph Phth Hphth 23 G = Q-16; X = O; NR5R6 = Piper Morph Phth Hphth 24 G = Q-17; X = O; NR5R6 = Piper Morph Phth Hphth 25 G = Q-1; X = S; NR5R6 = Piper Morph Phth Hphth 26 G = Q-2; X = S; NR5R6 = Piper Morph Phth Hphth 27 G = Q-3; X = S; NR5R6 = Piper Morph Phth Hphth 28 G = Q-4; X = S; NR5R6 = Piper Morph Phth Hphth 29 G = Q-5; X = S; NR5R6 = Piper Morph Phth Hphth 30 G = Q-6; X = S; NR5R6 = Piper Morph Phth Hphth 31 G = Q-7; X = S; NR5R6 = Piper Morph Phth Hphth 32 G = Q-9; X = S; NR5R6 = Piper Morph Phth Hphth 33 G = Q-10; X = S; NR5R6 = Piper Morph Phth Hphth 34 G = Q-15; X = S; NR5R6 = Piper Morph Phth Hphth 35 G = Q-16; X = S; NR5R6 = Piper Morph Phth Hphth 36 G = Q-17; X = S; NR5R6 = Piper Morph Phth Hphth TABLE 21 COLUMN 1 43 1 G = Q-1; X = NH; R18 = H Me i-Pr OH 2 G = Q-1; X = NH; R1 g = OMe SMe Ph (2,6-diF) Ph 3 G = Q-2; X = NH; R18 = H Me i-Pr OH 4 G = Q-2; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph =Q-3;5G NH;R18=HMei-PrOH= 6 G = Q-3; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 7 G = Q-4; X = NH; R18 = H Me i-Pr OH 8 G = Q-4; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 9 G = Q-5; X = NH; R18 = H Me i-Pr OH 10 G = Q-5; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph =Q-6;X=NH;R18=HMei-PrOH11G 12 G = Q-6; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 13 G = Q-7; X = NH; R18 = H Me i-Pr OH 14 G = Q-7; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 15 G = Q-9; X = NH; R18 = H Me i-Pr OH 16 G = Q-9; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 17 G = Q-10; X = NH ; R1 = H Me i-Pr OH 18 G = Q-10; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph =Q-15;19G NH;R18=HMei-PrOH= 20 G = Q-15; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph =Q-16;21G NH;R18=HMei-PrOH= 22 G = Q-16; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 23 G = Q-17; X = NH; R18 = H Me i-Pr OH 24 G = Q-17; X = NH; R18 = OMe SMe Ph (2,6-diF) Ph 25 G = Q-1; X = O; R18 = H Me Ph (2,6-diF) Ph 26 G = Q-2; X = O; R18 = H Me Ph (2,6-diF) Ph 27 G = Q-3; X = O; R18 = H Me Ph (2,6-diF) Ph 28 G = Q-4; X = O; R18 = H Me Ph (2,6-diF) Ph 29 G = Q-5; X = O ; R18 = H Me Ph (2,6-diF) Ph 30 G = Q-6; X = O ; R18 = H Me Ph (2,6-diF) Ph 31 G = Q-7; X = O; R18 = H Me Ph (2,6-diF) Ph 32 G = Q-9; X = O; R18= H Me Ph (2,6-diF) Ph 33 G = Q-10; X = O; R18 = H Me Ph (2,6-diF) Ph 34 G = Q-15; X = O; R18 = H Me Ph (2,6-diF) Ph 35 G = Q-16; X = O ; R18 = H Me Ph (2,6-diF) Ph 36 G = Q-17; X = O ; R18 = H Me Ph (2,6-diF) Ph 37 G = Q-1; X = S; R18 = H Me Ph (2,6-diF) Ph 38 G = Q-2; X = S; R18 = H Me Ph (2,6-diF) Ph 39 G = Q-3; X = S; R18 = H Me Ph (2,6-diF) Ph 40 G = Q-4; X = S; R18 = H Me Ph (2,6-diF) Ph 41 G = Q-5; X = S; R18 = H Me Ph (2,6-diF) Ph 42 G = Q-6; X = S; R18 = H Me Ph (2,6-diF) Ph 43 G = Q-7; X = S; R18 = H Me Ph (2,6-diF) Ph 44 G = Q-9; X = S; R18= H Me Ph (2,6-diF) Ph 45 G = Q-10; X = S; R18 = H Me Ph (2,6-diF) Ph 46 G = Q-15; X = S; R18= H Me Ph (2,6-diF) Ph 47 G = Q-16; X = S; R18= H Me Ph (2,6-diF) Ph 48 G = Q-17; X = S; R18 = H Me Ph (2,6-diF) Ph TABLE22 COLUMN 1 2 3 4 =Q-1;X=NH;R18=HClMei-Pr1G 2 G = Q-1; X = NH; R18 = OH OMe SMe S-n-Pr 3 G = Q-1; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph =Q-2;4G NH;R18=HClMei-Pr= 5 G = Q-2; X = NH; R18 OH OMe SMe S-n-Pr 6 G = Q-2; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 7 G = Q-3; X = NH; R18 = H C1 Me i-Pr 8 G = Q-3; X = NH; R18 = OH OMe SMe S-n-Pr 9 G = Q-3; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 10 G = Q-4; X = NH; R18 = H Cl Me i-Pr 11 G = Q-4; X = NH; R18 = OH OMe SMe S-n-Pr 12 G = Q-4; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 13 G = Q-5; X = NH ; R18= H Cl Me i-Pr 14 G = Q-5; X = NH; R18 = OH OMe SMe S-n-Pr 15 G = Q-5; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 16 G = Q-6; X = NH; R18 = H Cl Me i-Pr 17 G = Q-6; X = NH; R18 = OH OMe SMe S-n-Pr 18 G = Q-6; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph =Q-7;19G NH;R18=HClMei-Pr= =Q-7;20G NH;R18=OHOMeSMeS-n-Pr= 21 G = Q-7; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 22 G = Q-9; X = NH; R18 = H Cl Me i-Pr 23 G = Q-9; X = NH; R18 = OH OMe SMe S-n-Pr 24 G = Q-9; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 25 G = Q-10; X = NH; R18 = H Cl Me i-Pr 26 G = Q-10; X = NH; R18 = OH OMe SMe S-n-Pr 27 G = Q-10; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 28 G = Q-15; X = NH; R18 = H Cl Me i-Pr 29 G = Q-15; X = NH; R18 = OH OMe SMe S-n-Pr 30 G = Q-15; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 31 G = Q-16; X = NH; R18 = H Cl Me i-Pr 32 G = Q-16; X = NH; R18 = OH OMe SMe S-n-Pr 33 G = Q-16; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph =Q-17;34G NH;R18=HClMei-Pr= 35 G = Q-17; X = NH; R18 = OH OMe SMe S-n-Pr 36 G = Q-17; X = NH; R18 = SO2Me COMe Ph (2,6-diF) Ph 37 G = Q-1; X = O; R18 = H Me Ph (2,6-diF) Ph 38 G = Q-2; X = O; R18 = H Me Ph (2,6-diF) Ph 39 G = Q-3; X = O; R18 = H Me Ph (2,6-diF) Ph 40 G = Q-4; X = O; R18 = H Me Ph (2,6-diF) Ph 41 G = Q-5; X = O; R18 = H Me Ph (2,6-diF) Ph 42 G = Q-6; X = O; R18 = H Me Ph (2,6-diF) Ph 43 G = Q-7; X = O; R18 = H Me Ph (2,6-diF) Ph 44 G = Q-9; X = O; R18 = H Me Ph (2,6-diF) Ph 45 G = Q-10; X = O; R18 = H Me Ph (2,6-diF) Ph 46 G = Q-15; X = O; R18 = H Me Ph (2,6-diF) Ph 47 G = Q-16; X = O; R18 = H Me Ph (2,6-diF) Ph 48 G = Q-17; X = O; R18 = H Me Ph (2,6-diF) Ph 49 G = Q-1; X = S; R18 = H Me Ph (2,6-diF) Ph 50 G = Q-2; X = S; R18 = H Me Ph (2,6-diF) Ph 51 G = Q-3; X = S; R18 = H Me Ph (2,6-diF) Ph 52 G = Q-4; X = S; R18 = H Me Ph (2,6-diF) Ph 53 G = Q-5; X = S; R18 = H Me Ph (2,6-diF) Ph 54 G = Q-6; X = S; R18 = H Me Ph (2,6-diF) Ph 55 G = Q-7; X = S; R18 = H Me Ph (2,6-diF) Ph 56 G = Q-9; X = S; R18 = H Me Ph (2,6-diF) Ph 57 G = Q-10; X = S; R18 = H Me Ph (2,6-diF) Ph 58 G = Q-15; X = S; R18 = H Me Ph (2,6-diF) Ph 59 G = Q-16; X = S; R18= H Me Ph (2,6-diF) Ph 60 G = Q-17; X = S; R18 = H Me Ph (2,6-diF) Ph TABLE 23 COLUMN 3412 1 G = Q-1 ; X = NH; R18 = Me i-Pr t-Bu Ph =Q-1;X=NH;R18=(4-Cl)PhSO2MeCOMeCo-t-Bu2G 3 G = Q-1; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu =Q-2;4G NH;R18=Mei-Prt-BuPh= 5 G = Q-2; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 6 G = Q-2; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 7 G = Q-3; X = NH; R18 = Me i-Pr t-Bu Ph 8 G = Q-3; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 9 G = Q-3; X = NH; R18 = C02Me CONEt2 C02-t-Bu CONH-t-Bu 10 G = Q-4; X = NH; R18 = Me i-Pr t-Bu Ph 11 G = Q-4; X = NH; R18 = (4-Cl) Ph S02Me COMe CO-t-Bu 12 G = Q-4; X = NH; R18 = C02Me CONEt2 C02-t-Bu CONH-t-Bu 13 G = Q-5; X = NH; R18 = Me i-Pr t-Bu Ph 14 G = Q-5; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 15 G = Q-5; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 16 G = Q-6; X = NH; R18 = Me i-Pr t-Bu Ph 17 G = Q-6; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 18 G = Q-6; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 19 G = Q-7; X = NH; R18 = Me i-Pr t-Bu Ph 20 G = Q-7; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 21 G = Q-7; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 22 G = Q-9; X = NH; R18 = Me i-Pr t-Bu Ph 23 G = Q-9; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 24 G = Q-9; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 25 G = Q-10; X = NH; R18 = Me i-Pr t-Bu Ph 26 G = Q-10; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 27 G = Q-10; X = NH; R18 = C02Me CONEt2 C02-t-Bu CONH-t-Bu 28 G = Q-15; X = NIH; R18 = Me i-Pr t-Bu Ph 29 G = Q-15; X = NH; R18 = (4-Cl) Ph S02Me COMe CO-t-Bu 30 G = Q-15; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 31 G = Q-16; X = NH; R18 = Me i-Pr t-Bu Ph 32 G = Q-16; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 33 G = Q-16; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 34 G = Q-17; X = NH; R18 = Me i-Pr t-Bu Ph 35 G = Q-17; X = NH; R18 = (4-Cl)Ph SO2Me COMe CO-t-Bu 36 G = Q-17; X = NH; R18 = CO2Me CONEt2 CO2-t-Bu CONH-t-Bu 37 G = Q-1; X = O; R18 = Me i-Pr t-Bu Ph 38 G = Q-1; X = O; R18 = SO2Me CO-t-Bu CO2-t-Bu COHN-t-Bu 39 G = Q-2; X = O; R18 = Me i-Pr t-Bu Ph 40 G = Q-2; X = O; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 41 G = Q-3; X = O; R18 = Me i-Pr t-Bu Ph 42 G = Q-3; X = O; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 43 G = Q-4; X = O; R18 = Me i-Pr t-Bu Ph 44 G = Q-4; X = O; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 45 G = Q-5; X = O; R18 = Me i-Pr t-Bu Ph 46 G = Q-5; X = O; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 47 G = Q-6; X = O; R18 = Me i-Pr t-Bu Ph =Q-6;48G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-7;49G O;R18=Mei-Prt-BuPh= =Q-7;50G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-9;51G O;R18=Mei-Prt-BuPh= =Q-9;52G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-10;53G O;R18=Mei-Prt-BuPh= =Q-10;54G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-15;55G O;R18=Mei-Prt-BuPh= =Q-15;56G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-16;57G O;R18=Mei-Prt-BuPh= =Q-16;58G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-17;59G O;R18=Mei-Prt-BuPh= =Q-17;60G O;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= 61 G = Q-1; X=S; R18 = Me i-Pr t-Bu Ph =Q-1;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu62G =Q-2;X=S;R18=Mei-Prt-BuPh63G =Q-2;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu64G =Q-3;X=S;R18=Mei-Prt-BuPh65G =Q-3;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu66G =Q-4;X=S;R18=Mei-Prt-BuPh67G =Q-4;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu68G =Q-5;X=S;R18=Mei-Prt-BuPh69G =Q-5;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu70G 71 G = Q-6; X=S; R18 = Me i-Pr t-Bu Ph =Q-6;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu72G 73 G = Q-7; X=S; R18 = Me i-Pr t-Bu Ph 74 G = Q-7; X=S; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 75 G = Q-9; X=S; R18 = Me i-Pr i-Bu Ph =Q-9;X=S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu76G 77 G = Q-10; X=S; R18= Me i-Pr t-Bu Ph 78 G = Q-10; X=S; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 79 G = Q-15; X=S; R18 = Me i-Pr t-Bu Ph 80 G = Q-15; X=S; R18 = SO2Me CO-t-Bu CO2-t-Bu CONH-t-Bu 81 G = Q-16; X=S; R18 = Me i-Pr t-Bu Ph =Q-16;82G S;R18=SO2MeCO-t-BuCO2-t-BuCONH-t-Bu= =Q-17;83G S;R18=Mei-Prt-BuPh= 84 G = Q-17; X=S; R18 = SO@Me Co-t-Bu CO@-t-Bu CONH-t-Bu TABLE 24 (X = NH; Hal = I) COLUMN 1 2 3 4 5 6 1 G = Q-1 ; R6 = Me; R5 = H Me Et n-Pr i-Pr c-Pr 2 G = Q-1 ; R6 = Me; R5 = n-Bu i-Bu c-Pen n-Hex c-Hex Bn 3 G = Q-2 ; R6 = Me ; R5 = H Me Et n-Pr i-Pr c-Pr 4 G = Q-2 ; R6 = Me; R5 = n-Bu i-Bu c-Pen n-Hex c-Hex Bn 5 G = Q-3; R6 = Me; R5 = H Me Et n-Pr i-Pr c-Pr 6 G = Q-3; R6 = Me ; R5 = n-Bu i-Bu c-Pen n-Hex c-Hex Bn 7 G = Q-4 ; R6 = Me ; R5 = H Me Et n-Pr i-Pr c-Pr 8 G = Q-4; R6 = Me; R5 = n-Bu i-Bu c-Pen n-Hex c-Hex Bn 9 G = Q-5 ; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 10 G = Q-6; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 11 G = Q-7; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 12 G = Q-8 ; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 13 G = Q-9; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 14 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 15 G = Q-11 ; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 16 G = Q-12; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 17 G = Q-13; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 18 G = Q-14; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 19 G = Q-15; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 20 G = Q-16; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 21 G = Q-17 ; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 22 G = Q-1 ; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 23 G = Q-2 ; R6 = Ph ; R5 = H Me Et n-Pr n-Hex Bn 24 G = Q-3; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 25 G = Q-4; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 26 G = Q-5; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 27 G = Q-6; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 28 G = Q-7; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 29 G = Q-9; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 30 G = Q-10 ; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 31 G = Q-15; R6 = Ph ; R5 = H Me Et n-Pr n-Hex Bn 32 G = Q-1; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 33 G = Q-2; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 34 G = Q-3; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 35 G = Q-4; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 36 G = Q-5; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 37 G = Q-6; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 38 G = Q-7; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 39 G = Q-9; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 40 G = Q-10 ; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 41 G = Q-15; R6 = 2-Pyr; R5 = H Me Et n-Pr n-Hex Bn 42 G = Q-1 ; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 43 G = Q-2; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 44 G = Q-3; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 45 G = Q-4; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 46 G = Q-5; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 47 G = Q-6; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 48 G = Q-7; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 49 G = Q-9; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 50 G = Q-10 ; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 51 G = Q-15 ; R6 = 3-Pyr; R5 = H Me Et n-Pr n-Hex Bn 52 G = Q-l ; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 53 G = Q-2; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 54 G = Q-3; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 55 G = Q-4; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 56 G = Q-5; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 57 G = Q-6; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 58 G = Q-7; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 59 G = Q-9; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 60 G = Q-10 ; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 61 G = Q-15 ; R6 = 4-Pyr; R5 = H Me Et n-Pr n-Hex Bn 62 G = Q-1; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 63 G = Q-2; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 64 G = Q-3; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 65 G = Q-4; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 66 G = Q-5; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 67 G = Q-6; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 68 G = Q-7; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 69 G = Q-9; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn 70 G = Q-10 ; R6 = 2-Th ; R5 = H Me Et n-Pr n-Hex Bn 71 G = Q-15; R6 = 2-Th; R5 = H Me Et n-Pr n-Hex Bn (X = NH;Hal = Br) 72 G = Q-1 ; R6 = Me; R5 = H Me Et n-Pr i-Pr c-Pr 73 G = Q-2; R6 = Me; R5 = H Me Et n-Pr i-Pr c-Pr 74 G = Q-3; R6 = Me; R5 = H Me Et n-Pr i-Pr c-Pr 75 G = Q-4; R6 = Me; R5 = H Me Et n-Pr i-Pr c-Pr =Q-5;76G Me;R5=HMeEtn-Prn-HexBn= =Q-6;R6=Me;R5=HMeEtn-Prn-HexBn77G =Q-7;78G Me;R5=HMeEtn-Prn-HexBn= =Q-9;79G Me;R5=HMeEtn-Prn-HexBn= 80 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn =Q-15;81G Me;R5=HMeEtn-Prn-HexBn= (X = NH;Hal = Cl) =Q-1;82G Me;R5=HMeEtn-Pri-Prc-Pr= =Q-2;R6=Me;R5=HMeEtn-Pri-Prc-Pr83G =Q-3;R6=Me;R5=HMeEtn-Pri-Prc-Pr84G =Q-4;85G Me;R5=HMeEtn-Pri-Prc-Pr= =Q-5;86G Me;R5=HMeEtn-Prn-HexBn= =Q-6;87G Me;R5=HMeEtn-Prn-HexBn= =Q-7;88G Me;R5=HMeEtn-Prn-HexBn= =Q-9;R6=Me;R5=HMeEtn-Prn-HexBn89G =Q-10;R6=Me;R5=HMeEtn-Prn-HexBn90G =Q=15;91G Me;R5=HMeEtn-Prn-HexBn= TABLE 25 (X = O ; Hal = I) COLUMN 345612 =Q-1;R6=Me;R5=HMeEtn-Prn-HexBn1G =Q-2;R6=Me;R5=HMeEtn-Prn-HexBn2G =Q-3;3G Me;R5=HMeEtn-Prn-HexBn= =Q-4;R6=Me;R5=HMeEtn-Prn-HexBn4G =Q-5;R6=Me;R5=HMeEtn-Prn-HexBn5G =Q-6;6G Me;R5=HMeEtn-Prn-HexBn= =Q-7;7G Me;R5=HMeEtn-Prn-HexBn= =Q-9;8G Me;R5=HMeEtn-Prn-HexBn= =Q-10;9G Me;R5=HMeEtn-Prn-HexBn= =Q-15;10G Me;R5=HMeEtn-Prn-HexBn= =Q-1;11G Ph;R5=HMeEtn-Prn-HexBn= 12 G = Q-2; R6 = Ph ; R5= H Me Et n-Pr n-Hex Bn 13 G = Q-3; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn =Q-4;R6=Ph;R5=HMeEtn-PRn-HexBn14G 15 G = Q-5; R6 = Ph ; R5= H Me Et n-Pr n-Hex Bn 16 G = Q-6; R6 = Ph ; R5= H Me Et n-Pr n-Hex Bn 17 G = Q-7; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 18 G = Q-9; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 19 G = Q-10 ; R6 = Ph ; R5 = H Me Et n-Pr n-Hex Bn =Q-15;20G Ph;R5=HMeEtn-Prn-HexBn= (X = 0;Hal = Br) 21 G = Q-1; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 22 G = Q-2; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 23 G = Q-3; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 24 G = Q-4; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 25 G = Q-5; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 26 G = Q-6; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 27 G = Q-7; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 28 G = Q-9; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 29 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 30 G = Q-15; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn (X = O; Hal = Cl) 31 G = Q-1; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 32 G = Q-2; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 33 G = Q-3; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 34 G = Q-4; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 35 G = Q-5; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 36 G = Q-6; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 37 G = Q-7 ; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 38 G = Q-9; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 39 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 40 G = Q-15; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn TABLE 26 (X = S; Hal = I) COLUMN 1 2 3 4 5 6 1 G = Q-1; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 2 G = Q-2; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 3 G = Q-3; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 4 G = Q-4; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 5 G = Q-5; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 6 G = Q-6; R6 = Me ; R5 = H Me Et n-Pr n-Hex Bn 7 G = Q-7; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 8 G = Q-9; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 9 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 10 G = Q-15; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 11 G = Q-1; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 12 G = Q-2; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 13 G = Q-3; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 14 G = Q-4; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 15 G = Q-5; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 16 G = Q-6 ; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 17 G = Q-7; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 18 G = Q-9; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 19 G = Q-10; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn 20 G = Q-15; R6 = Ph; R5 = H Me Et n-Pr n-Hex Bn (X = S;Hal = Br) 21 G = Q-1; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 22 G = Q-2; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 23 G = Q-3; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 24 G = Q-4; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 25 G = Q-5; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 26 G = Q-6; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 27 G = Q-7; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 28 G = Q-9; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 29 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 30 G = Q-15; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn (X = S; Hal = Cl) 31 G = Q-1; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 32 G = Q-2; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 33 G = Q-3; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 34 G = Q-4; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 35 G = Q-5; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 36 G = Q-6; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 37 G = Q-7; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 38 G = Q-9; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 39 G = Q-10; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn 40 G = Q-15; R6 = Me; R5 = H Me Et n-Pr n-Hex Bn Formulation/Utility Compounds of this invention will generally be used as a formulation or composition with an agriculturally suitable carrier comprising at least one of a liquid diluent, a solid diluent or a surfactant. The formulation or composition ingredients are selected to be

consistent with the physical properties of the active ingredient, mode of application and environmental factors such as soil type, moisture and temperature. Useful formulations include liquids such as solutions (including emulsifiable concentrates), suspensions, emulsions (including microemulsions and/or suspoemulsions) and the like which optionally can be thickened into gels. Useful formulations further include solids such as dusts, powders, granules, pellets, tablets, films, and the like which can be water-dispersible ("wettable") or water-soluble. Active ingredient can be (micro) encapsulated and further formed into a suspension or solid formulation; alternatively the entire formulation of active ingredient can be encapsulated (or"overcoated"). Encapsulation can control or delay release of the active ingredient. Sprayable formulations can be extended in suitable media and used at spray volumes from about one to several hundred liters per hectare. High-strength compositions are primarily used as intermediates for further formulation.

The formulations will typically contain effective amounts of active ingredient, diluent and surfactant within the following approximate ranges which add up to 100 percent by weight.

Weight Percent Active Ingrédient Diluent Surfactant Water-Dispersible and Water-soluble 5-90 0-94 1-15 Granules, Tablets and Powders.

Suspensions, Emulsions, Solutions 5-50 40-95 0-15 (including Emulsifiable Concentrates) Dusts 1-25 70-99 0-5 Granules and Pellets 0.01-99 5-99.99 0-15 High Strength Compositions 90-99 0-10 0-2 Typical solid diluents are described in Watkins, et al., Handbook of Insecticide Dust Diluents and Carriers, 2nd Ed., Dorland Books, Caldwell, New Jersey. Typical liquid diluents are described in Marsden, Solvents Guide, 2nd Ed., Interscience, New York, 1950.

McCutcheon's Detergents and Emulsifiers Annual, Allured Publ. Corp., Ridgewood, New Jersey, as well as Sisely and Wood, Encyclopedia of Surface Active Agents, Chemical Publ.

Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foam, caking, corrosion, microbiological growth and the like, or thickeners to increase viscosity.

Surfactants include, for example, polyethoxylated alcohols, polyethoxylated alkylphenols, polyethoxylated sorbitan fatty acid esters, dialkyl sulfosuccinates, alkyl sulfates, alkylbenzene sulfonates, organosilicones, N, N-dialkyltaurates, lignin sulfonates, naphthalene sulfonate formaldehyde condensates, polycarboxylates, and polyoxyethylene/polyoxypropylene block copolymers. Solid diluents include, for example,

clays such as bentonite, montmorillonite, attapulgite and kaolin, starch, sugar, silica, talc, diatomaceous earth, urea, calcium carbonate, sodium carbonate and bicarbonate, and sodium sulfate. Liquid diluents include, for example, water, N, N-dimethylformamide, dimethyl sulfoxide, N-alkylpyrrolidone, ethylene glycol, polypropylene glycol, paraffins, alkylbenzenes, alkylnaphthalenes, oils of olive, castor, linseed, tung, sesame, corn, peanut, cotton-seed, soybean, rape-seed and coconut, fatty acid esters, ketones such as cyclohexanone, 2-heptanone, isophorone and 4-hydroxy-4-methyl-2-pentanone, and alcohols such as methanol, cyclohexanol, decanol and tetrahydrofurfuryl alcohol.

Solutions, including emulsifiable concentrates, can be prepared by simply mixing the ingredients. Dusts and powders can be prepared by blending and, usually, grinding as in a hammer mill or fluid-energy mill. Suspensions are usually prepared by wet-milling; see, for example, U. S. 3,060,084. Granules and pellets can be prepared by spraying the active material upon preformed granular carriers or by agglomeration techniques. See Browning, "Agglomeration", Chemical Engineering, December 4,1967, pp 147-48, Perry's Chemical Engineer's Handbook, 4th Ed., McGraw-Hill, New York, 1963, pages 8-57 and following, and WO 91/13546. Pellets can be prepared as described in U. S. 4,172,714.

Water-dispersible and water-soluble granules can be prepared as taught in U. S. 4,144,050, U. S. 3,920,442 and DE 3,246,493. Tablets can be prepared as taught in U. S. 5,180,587, U. S.

5,232,701 and U. S. 5,208,030. Films can be prepared as taught in GB 2,095,558 and U. S.

3,299,566.

For further information regarding the art of formulation, see U. S. 3,235, 361, Col. 6, line 16 through Col. 7, line 19 and Examples 10-41; U. S. 3,309,192, Col. 5, line 43 through Col. 7, line 62 and Examples 8,12,15,39,41,52,53,58,132,138-140,162-164,166,167 and 169-182; U. S. 2,891,855, Col. 3, line 66 through Col. 5, line 17 and Examples 1-4; Klingman, Weed Control as a Science, John Wiley and Sons, Inc., New York, 1961, pp 81-96; and Hance et al., Weed Control Handbook, 8th Ed., Blackwell Scientific Publications, Oxford, 1989.

In the following Examples, all percentages are by weight and all formulations are prepared in conventional ways. Compound numbers refer to compounds in Index Tables A-B.

Example A Wettable Powder Compound 2 65.0% dodecylphenol polyethylene glycol ether 2.0% sodium ligninsulfonate 4.0% sodium silicoaluminate 6.0% montmorillonite (calcined) 23.0%.

Example B Granule Compound 4 10.0% attapulgite granules (low volatile matter, 0.71/0.30 mm; U. S. S. No. 25-50 sieves) 90.0%.

Example C Extruded Pellet Compound 2 25.0% anhydrous sodium sulfate 10.0% crude calcium ligninsulfonate 5.0% sodium alkylnaphthalenesulfonate 1.0% calcium/magnesium bentonite 59.0%.

Example D Emulsifiable Concentrate Compound 4 20.0% blend of oil soluble sulfonates and polyoxyethylene ethers 10.0% isophorone 70.0%.

The compounds of this invention exhibit activity against a wide spectrum of foliar-feeding, fruit-feeding, stem or root feeding, seed-feeding, aquatic and soil-inhabiting arthropods (term"arthropods"includes insects, mites and nematodes) which are pests of growing and stored agronomic crops, forestry, greenhouse crops, ornamentals, nursery crops, stored food and fiber products, livestock, household, and public and animal health. Those skilled in the art will appreciate that not all compounds are equally effective against all growth stages of all pests. Nevertheless, all of the compounds of this invention display activity against pests that include: eggs, larvae and adults of the Order Lepidoptera; eggs, foliar-feeding, fruit-feeding, root-feeding, seed-feeding larvae and adults of the Order Coleoptera; eggs, immatures and adults of the Orders Hemiptera and Homoptera; eggs, larvae, nymphs and adults of the Order Acari; eggs, immatures and adults of the Orders Thysanoptera, Orthoptera and Dermaptera; eggs, immatures and adults of the Order Diptera; and eggs, juveniles and adults of the Phylum Nematoda. The compounds of this invention are also active against pests of the Orders Hymenoptera, Isoptera, Siphonaptera, Blattaria, Thysanura and Psocoptera; pests belonging to the Class Arachnida and Phylum Platyhelminthes. Specifically, the compounds are active against southern corn rootworm (Diabrotica undecimpunctata howardi), aster leafhopper (Mascrosteles fascifrons), boll weevil (Anthonomus grandis), two-spotted spider mite (Tetranychus urticae), fall armyworm (Spodoptera frugiperda), black bean aphid (Aphis fabae), green peach aphid (Myzus persica), cotton aphid (Aphis gossypii), Russian wheat aphid (Diuraphis noxia), English grain aphid

(Sitobion avenae), tobacco budworm (Heliothis virescens), rice water weevil (Lissorhoptrus oryzophilus), rice leaf beetle (Oulema oryzae), whitebacked planthopper (Sogatella furcifera), green leafhopper (Nephotettix cincticeps), brown planthopper (Nilaparvata lugens), small brown planthopper (Laodelphax striatellus), rice stem borer (Chilo suppressalis), rice leafroller (Cnaphalocrocis medinalis), black rice stink bug (Scotinophara lurida), rice stink bug (Oebalus pugnax), rice bug (Leptocorisa chinensis), slender rice bug (Cletus puntiger), and southern green stink bug (Nezara viridula). The compounds are active on mites, demonstrating ovicidal, larvicidal and chemosterilant activity against such families as Tetranychidae including Tetranychus urticae, Tetranychus cinnabarinus, Tetranychus mcdanieli, Tetranychus pacificus, Tetranychus turkestani, Byrobia rubrioculus, Panonychus ulmi, Panonychus citri, Eotetranychus carpini borealis, Eotetranychus, hicoriae, Eotetranychus sexmaculatus, Eotetranychus yumensis, Eotetranychus banksi and Oligonychus pratensis; Tenuipalpidae including Brevipalpus lewisi, Brevipalpus phoenicis, Brevipalpus californicus and Brevipalpus obovatus; Eriophyidae including Phyllocoptruta oleivora, Eriophyes sheldoni, Aculus cornutus, Epitrimerus pyri and Eriophyes mangiferae.

See WO 90/10623 and WO 92/00673 for more detailed pest descriptions.

The compounds of this invention are also useful as plant disease control agents. The present invention therefore further comprises a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof to be protected, or to the plant seed or seedling to be protected, an effective amount of a compound of the invention or a fungicidal composition containing said compound. The compounds and compositions of this invention provide control of diseases caused by a broad spectrum of fungal plant pathogens in the Basidiomycete, Ascomycete, Oomycete and Deuteromycete classes. They are effective in controlling a broad spectrum of plant diseases, particularly foliar pathogens of ornamental, vegetable, field, cereal, and fruit crops. These pathogens include Plasmopara viticola, Phytophthora infestans, Peronospora tabacina, Pseudoperonospora cubensis, Pythium aphanidermatum, Alternaria brassicae, Septoria nodorum, Septoria tritici, Cercosporidium personatum, Cercospora arachidicola, Pseudocercosporella herpotrichoides, Cercospora beticola, Botrytis cinerea, Monilinia fructicola, Pyricularia oryzae, Podosphaera leucotricha, Venturia inaequalis, Erysiphe graminis, Uncinula necatur, Puccinia recondita, Puccinia graminis, Hemileia vastatrix, Puccinia striiformis, Puccinia arachidis, Rhizoctonia solani, Sphaerotheca fuliginea, Fusarium oxysporum, Verticillium dahliae, Pythium aphanidermatum, Phytophthora megasperma, Sclerotinia sclerotiorum, Sclerotium rolfsii, Erysiphe polygoni, Pyrenophora teres, Gaeumannomyces graminis, Rynchosporium secalis, Fusarium roseum, Bremia lactucae and other generea and species closely related to these pathogens.

Compounds of this invention can also be mixed with one or more other insecticides, fungicides, nematocides, bactericides, acaricides, growth regulators, chemosterilants,

semiochemicals, repellents, attractants, pheromones, feeding stimulants or other biologically active compounds to form a multi-component pesticide giving an even broader spectrum of agricultural protection. Examples of such agricultural protectants with which compounds of this invention can be formulated are: insecticides such as abamectin, acephate, azinphos-methyl, bifenthrin, buprofezin, carbofuran, chlorfenapyr, chlorpyrifos, chlorpyrifos-methyl, cyfluthrin, beta-cyfluthrin, cyhalothrin, lambda-cyhalothrin, deltamethrin, diafenthiuron, diazinon, diflubenzuron, dimethoate, esfenvalerate, fenoxycarb, fenpropathrin, fenvalerate, fipronil, flucythrinate, tau-fluvalinate, fonophos, imidacloprid, isofenphos, malathion, metaldehyde, methamidophos, methidathion, methomyl, methoprene, methoxychlor, methyl 7-chloro-2, 5-dihydro-2-[[N-(methoxycarbonyl)-N-[4- (trifluoromethoxy) phenyl] amino] carbonyl] indeno [1, 2-e] [1, 3, 4] oxadiazine-4a (3H)- carboxylate (DPX-JW062), monocrotophos, oxamyl, parathion, parathion-methyl, permethrin, phorate, phosalone, phosmet, phosphamidon, pirimicarb, profenofos, rotenone, sulprofos, tebufenozide, tefluthrin, terbufos, tetrachlorvinphos, thiodicarb, tralomethrin, trichlorfon and triflumuron; fungicides such as azoxystrobin, benomyl, blasticidin-S, Bordeaux mixture (tribasic copper sulfate), bromuconazole, captafol, captan, carbendazim, chloroneb, chlorothalonil, copper oxychloride, copper salts, cymoxanil, cyproconazole, cyprodinil (CGA 219417), diclomezine, dicloran, difenoconazole, dimethomorph, diniconazole, diniconazole-M, dodine, edifenphos, epoxiconazole (BAS 480F), famoxadone, fenarimol, fenbuconazole, fenpiclonil, fenpropidin, fenpropimorph, fluazinam, fluquinconazole, flusilazole, flutolanil, flutriafol, folpet, fosetyl-aluminum, furalaxyl, hexaconazole, ipconazole, iprobenfos, iprodione, isoprothiolane, kasugamycin, kresoxim-methyl, mancozeb, maneb, mepronil, metalaxyl, metconazole, S-methyl 7-benzothiazolecarbothioate (CGA 245704), myclobutanil, neo-asozin (ferric methanearsonate), oxadixyl, penconazole, pencycuron, probenazole, prochloraz, propiconazole, pyrifenox, pyroquilon, quinoxyfen, spiroxamine (KWG4168), sulfur, tebuconazole, tetraconazole, thiabendazole, thiophanate-methyl, thiram, triadimefon, triadimenol, tricyclazole, triticonazole, validamycin and vinclozolin; nematocides such as aldoxycarb and fenamiphos; bactericides such as streptomycin; acaricides such as amitraz, chinomethionat, chlorobenzilate, cyhexatin, dicofol, dienochlor, etoxazole, fenazaquin, fenbutatin oxide, fenpropathrin, fenpyroximate, hexythiazox, propargite, pyridaben and tebufenpyrad; and biological agents such as Bacillus thuringiensis, Bacillus thuringiensis delta endotoxin, baculovirus, and entomopathogenic bacteria, virus and fungi.

In certain instances, combinations with other fungicides or arthropodicides having a similar spectrum of control but a different mode of action will be particularly advantageous for resistance management.

Preferred for better control of pests (use rate or spectrum) or resistance management are mixtures of a compound of this invention with an arthropodicide selected from the group:

acephate, buprofezin, carbofuran, 2,5-dihydro-2-[[N-(methoxycarbonyl)-N-[4- (trifluoromethoxy) phenyl] amino] carbonyl] indeno [1, 2-e] [1, 3, 4] oxadiazine-4a (3H)- carboxylate (DPX-JW062), dimethoate, esfenvalerate, fipronil, imidacloprid, methomyl, monocrotophos, phorate, and phosphamidon.

Arthropod pests are controlled and protection of agronomic, horticultural and specialty crops, animal and human health is achieved by applying one or more of the compounds of this invention, in an effective amount, to the environment of the pests including the agronomic and/or nonagronomic locus of infestation, to the area to be protected, or directly on the pests to be controlled. Thus, the present invention further comprises a method for the control of foliar and soil inhabiting arthropods and nematode pests and protection of agronomic and/or nonagronomic crops, comprising applying one or more of the compounds of the invention, or compositions containing at least one such compound, in an effective amount, to the environment of the pests including the agronomic and/or nonagronomic locus of infestation, to the area to be protected, or directly on the pests to be controlled. A preferred method of application is by spraying. Alternatively, granular formulations of these compounds can be applied to the plant foliage or the soil. Other methods of application include direct and residual sprays, aerial sprays, seed coats, microencapsulations, systemic uptake, baits, eartags, boluses, foggers, fumigants, aerosols, dusts and many others. The compounds can be incorporated into baits that are consumed by the arthropods or in devices such as traps and the like.

For the control arthropod pests, the compounds of this invention can be applied in their pure state, but most often application will be of a formulation comprising one or more compounds with suitable carriers, diluents, and surfactants and possibly in combination with a food depending on the contemplated end use. A preferred method of application involves spraying a water dispersion or refined oil solution of the compounds. Combinations with spray oils, spray oil concentrations, spreader stickers, adjuvants, other solvents, and synergists such as piperonyl butoxide often enhance compound efficacy.

The rate of application required for effective control will depend on such factors as the species of arthropod to be controlled, the pest's life cycle, life stage, its size, location, time of year, host crop or animal, feeding behavior, mating behavior, ambient moisture, temperature, and the like. Under normal circumstances, application rates of about 0.01 to 2 kg of active ingredient per hectare are sufficient to control pests in agronomic ecosystems, but as little as 0.001 kg/hectare may be sufficient or as much as 8 kg/hectare may be required. For nonagronomic applications, effective use rates will range from about 1.0 to 50 mg/square meter but as little as 0.1 mg/square meter may be sufficient or as much as 150 mg/square meter may be required.

Plant disease control is ordinarily accomplished by applying an effective amount of a compound of this invention either pre-or post-infection, to the portion of the plant to be

protected such as the roots, stems, foliage, fruit, seeds, tubers or bulbs, or to the media (soil or sand) in which the plants to be protected are growing. The compounds can also be applied to the seed to protect the seed and seedling.

For plant disease control, rates of application for these compounds can be influenced by many factors of the environment and should be determined under actual use conditions.

Foliage can normally be protected when treated at a rate of from less than 1 g/ha to 5,000 g/ha of active ingredient. Seed and seedlings can normally be protected when seed is treated at a rate of from 0.1 to 10 g per kilogram of seed.

The following tests demonstrate the control efficacy of compounds of this invention on specific arthropod and pathogen pests. For the tests on arthropod pests,"control efficacy" represents inhibition of arthropod development (including mortality) that causes significantly reduced feeding. The arthropod and pathogen pest control protection afforded by the compounds is not limited, however, to these species. See Index Tables A-D for compound descriptions. The abbreviation"Ex."stands for"Example"and is followed by a number indicating in which example the compound is prepared. Isomer indicates cis or trans with respect to the cyclohexane ring.

INDEX TABLE A Cmpd No. Isomer R7 R5 G mp (°C) (Ex.No.) 1 (Ex. 1) cis H H 6-Et-5-CI-4-119-121 pyrimidinyl 2 trans H H 6-Et-5-CI-4-> 255 a pyrimidinyl 3 cis: trans = 7.5: 1 H H 4-quinazolinyl solid a 4 trans H H 4-quinazolinyl > 260 a 5 cis H H 6-MeOCH2-5-109-111 MeO-4- pyrimidinyl <BR> <BR> <BR> 6 cis : trans = 18: 1 H H 6-MeOCH2-4-solid a pyrimidinyl <BR> <BR> <BR> 7 cis H H 5, 6, 7, 8- solid a tetrahydro-4- quinazolinyl 8 cis H H 6-Et-4-123-124 pyrimidinyl Cmpd No. Isomer R7 R5 G m (°C) Ex. No.

9 cis H H 3-t-Bu-1,2,4- 175-180 thiadiazol-5-yl 10 (Ex. 2a) cis H Me 6-Et-5-CI-4-68-70 pyrimidinyl 11 cis H Et 6-Et-5-CI-4-oil a pyrimidinyl 12 cis H n-Pr 6-Et-5-CI-4-81-83 pyrimidinyl 13 cis H n-Bu 6-Et-5-CI-4-oil a pyrimidinyl 14 cis H CH2CH=CH2 6-Et-5-CI-4-oil a pyrimidinyl 15 (Ex. 2b) cis Me Me 6-Et-5-Cl-4- 86-87 pyrimidinyl 16 cis Et Et 6-Et-5-CI-4-99-100 pyrimidinyl 17 cis CH2CH=CH2 CH2CH=CH2 6-Et-5-Cl-5- oil a pyrimidinyl 18 (Ex. 3) cis H#HCl H#HCl 6-Et-5-Cl-4- 239-242 pyrimidinyl a See Index Table D for 1H NMR data.

INDEX TABLE B IsomerR7R5R6mp(°C)CmpdNo.

HCOMeH158-15919cis MeCOMeH126-133a20cis HCO2-t-BuH152-15421cis MeCO2-t-BuH121-12722cis EtCO2-t-BuHoila23cis <BR> <BR> CH2C#CHCO2-t-BuHsolida24cis IsomerR7R5R6mp(°CCmpdNo. <BR> <BR> <BR> <BR> <P>25 cis H C02Bn H oil a 26 (Ex. HOMeHoilacis <BR> <BR> <BR> <BR> 27 (Ex. llb) trans H OMe H 87-88 28 cis Me OMe H oil a <BR> <BR> <BR> <BR> 29 cis: trans = 7: 1 H OBn H oil a<BR> <BR> <BR> <BR> <BR> <BR> <BR> 30 trans H OBn H 116-121 31 (Ex. 7a) cis H Me Me 62-66 32 (Ex. 7b) trans H Me Me oil a <BR> <BR> <BR> <BR> 33 cis H n-Bu Me oil a<BR> <BR> <BR> <BR> <BR> <BR> <BR> 34 trans H n-Bu Me 47-48<BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> 35 cis Me C02Et Me oil a HOMeMeoila36cis <BR> <BR> <BR> <BR> 37 (Ex. 5a) cis H H Ph 88-93 38 (Ex. 5b) trans H H Ph 137-139 HMePhoila39cis 40 trans: cis = 8: 1 H Me Ph 83-84a <BR> <BR> <BR> <BR> 41 trans: cis = H Et Ph oil a 1.3: 1 =2:1HBnPhoila42cis:trans <BR> <BR> <BR> <BR> 43 trans H Bn Ph oil a<BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> 44 cis: trans = H CH2CH=CH2 Ph oil a 1.5: 1 45 trans : cis = 6: 1 H CH2CH=CH2 Ph oil a 46 (Ex. 6) cis H CH2C#CH Ph oila <BR> <BR> <BR> 47 cis H CH2CN Ph 79-80<BR> <BR> <BR> <BR> <BR> <BR> <BR> 48 cis H (CH2) 20H Ph 111-115<BR> <BR> <BR> <BR> <BR> <BR> <BR> 49 trans H (CH2) 20H Ph solid a<BR> <BR> <BR> <BR> <BR> <BR> <BR> 50 cis H CH2CO2-t-Bu Ph solid a HCOMePh125-12751cis HCOEtPh86-9052cis <BR> <BR> <BR> <BR> 53 cis H COCF3 Ph 99-101 HCO-c-PrPhoila54cis 55 cis H CO-t-Bu Ph 80-81 HCOPhPh134-13656cis <BR> <BR> <BR> <BR> 57 cis H C02Me Ph 95<BR> <BR> <BR> <BR> <BR> <BR> <BR> 58 cis H C02Et Ph oil a<BR> <BR> <BR> <BR> <BR> <BR> <BR> 59 trans H C02Et Ph 137-140<BR> <BR> <BR> <BR> <BR> <BR> <BR> 60 cis H C02-i-Pr Ph 72-75<BR> <BR> <BR> <BR> <BR> <BR> <BR> 61 cis H C02-t-Bu Ph oil a<BR> <BR> <BR> <BR> <BR> <BR> <BR> 62 cis H C02Bn Ph 88-89 HCONMe2Phoila63cis <BR> <BR> <BR> 64 cis H S02CF3 Ph 93-94<BR> <BR> <BR> <BR> <BR> <BR> 65 cis H S02Ph Ph solid a IsomerR7R5R6mp(°CCmpdNo.

66 (Ex. 12) cis H OMe COMe oil a 67 cis H OBn COMe 132-134 68 cis H H 2, 6-diCI-4-CF3-Ph 71-72 69 cis H H 3-CI-5-CF3-2-91-92 pyridinyl 70 (Ex. 2c) cis Me Me 5-Cl-6-i-Pr-4- 95-97 pyrimidinyl 71 (Ex. 9) cis H H 6-MeOCH2-5-MeO-> 104 a 4-pyrimidinyl 72 (Ex. 4) cis H H 4-quinazolinyl 188-191 73 cis H H 3-t-Bu-1,2, 4- solida thiadiazol-5-yl a See Index Table D for 1H NMR data.

INDEX TABLE C CmpdCmpdNo. Isomer mp(°CNR5R6 74 cis: trans= 1.4: 1 H 1-piperidinyl solida 75 cis H 1-pyrrolidinyl 95-97 H1-pyrrolidinyl59-6276trans <BR> <BR> <BR> 77 cis H 4-morpholinyl 145-146<BR> <BR> <BR> <BR> 78 trans H 4-morpholinyl 141-146<BR> <BR> <BR> <BR> 79 cis H 4-Me-1-piperazinyl oil a<BR> <BR> <BR> <BR> 80 trans H 4-Me-1-piperazinyl 85-89<BR> <BR> <BR> <BR> 81 cis H 4-Et-1-piperazinyl oil a<BR> <BR> <BR> <BR> 82 trans H 4-Et-1-piperazinyl 91-96<BR> <BR> <BR> <BR> 83 cis H 4-(C6H5CH2)-1-piperazinyl oil a H4-(C6H5CH2)-1-piperazinyl88-8984trans <BR> <BR> 85 cis H 4- (C6H5)-1-piperazinyl 105-108<BR> <BR> <BR> <BR> 86 trans H 4- (C6H5)-1-piperazinyl 115-120<BR> <BR> <BR> <BR> 87 cis H 4- (4-F-C6H5)-1-piperazinyl 93-94<BR> <BR> <BR> <BR> 88 trans H 4- (4-F-C6H5)-1-piperazinyl 70-72 H4-(2-pyridinyl)-1-piperazinyl130-137a89cis Cmpd No. Isomer R7 NR5 R6 mp °C 90 trans: cis = 10 : 1 H 4-(2-pyridinyl)-1-piperazinyl 100-103a 91 cis H 0 145-154 a -N / O 92 cis H 0 157-160 (Ex. 10) N O 93 cis H Me 217-221 (Ex. 8) N I Me Me Me 94 trans H Me 194-197 Me/Me 95 cis H Et 106-110 \ Me 96 cis H Me 61-64 '6' a See Index Table D for 1H NMR data.

INDEX TABLE D Cmpd Isomer 1H NMR Data b No.

2 8 (CF3CO2D) 8.57 (s, 2H), 4. 36 (m, 2H), 2.99 (q, 4H), 2.26 (m, 4H), 1.71 (m, 4H), 1.36 (t, 6H).

3 cis 8 (DMSO-d6) 8.50 (s, 2H), 8.43 (dd, 2H), 7.81 (d, 2H), 7.77 (ddd, 2H), 7.68 (dd, 2H), 7.52 (ddd, 2H), 4.32 (m, 2H), 2.09 (m, 4H), 1.80 (m, 4H).

4 trans 8 (CF3CO2D) 8.92 (s, 2H), 8.35 (d, 2H), 8.15 (t, 2H), 7.91 (m, 4H), 4.70 (m, 2H), 2.47 (m, 4H), 1.98 (m, 4H).

6 cis 8 8.48 (s, 2H), 6.47 (s, 2H), 5.04 (br s, 2H), 4.40 (s, 4H), 3.92 (br s, 2H), 3.49 (s, 6H), 1.92 (m, 4H), 1.72 (m, 4H).

7 cis 6 8.42 (s, 2H), 4.50 (d, 2H), 4.25 (m, 2H), 2.71 (t, 4H), 2.33 (t, 4H), 2.06-1.62 (m, 16H).

Cmpd Isomer 1H NMR Data b No.

11 cis 5 8.48 (s, 1H), 8.43 (s, 1H), 5.63 (d, 1H), 4.34 (m, 1H), 4.03 (m, 1H), 3.55 (q, 2H), 2.87 (q, 2H), 2.81 (q, 2H), 2.13-1.65 (m, 8H), 1.29 (t, 3H), 1.28 (t, 3H), 1.16 (t, 3H).

13 cis 8 8.48 (s, 1H), 8.43 (s, 1H), 5.61 (d, 1H), 4.33 (m, 1H), 3.98 (m, 1H), 3.45 (m, 2H), 2.87 (q, 2H), 2.81 (q, 2H), 2.14-1.64 (m, 8H), 1.50 (m, 2H), 1.32 (m, 2H), 1.29 (t, 3H), 1.28 (t, 3H), 0.91 (t, 3H).

14 cis 6 8.49 (s, 1H), 8.42 (s, 1H), 5.92 (ddt, 1H), 5.64 (d, 1H), 5.21 (dq, 1H), 5.12 (dq, 1H), 4.35 (m, 1H), 4.15 (dt, 2H), 4.00 (m, 1H), 2.87 (q, 2H), 2.81 (q, 2H), 2.04 (m, 4H), 1.85-1.63 (m, 4H), 1.29 (t, 3H), 1.28 (t, 3H).

17 cis 8 8.56 (s, 2H), 5.79 (m, 2H), 5.13 (m, 2H), 5.06 (m, 2H), 4.08 (m, 6H), 2.89 (q, 4H), 2.01 (m, 4H), 1.56 (m, 4H), 1. 30 (t, 6H).

20 cis 8 8.44 (s, 1H), 5.68 (br d, 1H), 4.12 (m, 2H), 3.01 (s, 3H), 2.85 (q, 2H), 2.04 (s, 3H), 1.96 (m, 2H), 1.73 (m, 6H), 1.28 (t, 3H).

23 cis 6 8.46 (s, 1H), 4.78 (br s, 1H), 4.02 (m, 1H), 3.82 (m, 1H), 3.54 (q, 2H), 2.86 (q, 2H), 1.97-1.53 (m, 8H), 1.47 (s, 9H), 1.28 (t, 3H), 1.12 (t, 3H).

24 cis 8 8.56 (s, 1H), 4.72 (br s, 1H), 4.24 (d, 2H), 4.15 (m, 1H), 3.80 (m, 1H), 2.89 (q, 2H), 2.19 (t, 1H), 1.98-1.56 (m, 8H), 1.47 (s, 9H), 1.29 (t, 3H).

25 cis 6 8.40 (s, 1H), 7.35 (m, 5H), 5. 34 (d, 1H), 5.10 (s, 2H), 4.98 (br s, 1H), 4.13 (m, 1H), 3.78 (m, 1H), 2.77 (q, 2H), 1.84 (m, 4H), 1.68 (m, 4H), 1.25 (t, 3H).

26 cis 8 8.41 (s, 1H), 5.47 (br s, 1H), 5.42 (br d, 1H), 4.18 (m, 1H), 3.58 (s, 3H), 3.07 (m, 1H), 2.78 (q, 2H), 1.87-1.55 (m, 8H), 1.26 (t, 3H).

28 cis 8 8.43 (s, 1H), 5.43 (br s, 1H), 4.15 (d, 1H), 3.59 (s, 3H), 3.17 (m, 1H), 3.00 (s, 3H), 2.85 (q, 2H), 2.06-1.87 (m, 4H), 1.61 (m, 4H), 1.28 (t, 3H).

29 cis 8 8.40 (s, 1H), 7.39-7.23 (m, 5H), 5.46 (br s, 1H), 5.40 (d, 1H), 4.73 (s, 2H), 4.17 (m, 1H), 3.12 (m, 1H), 2.78 (q, 2H), 1.82-1.57 (m, 8H), 1. 26 (t, 3H).

32 trans 8 8.40 (s, 1H), 5.19 (d, 1H), 3.94 (m, 1H), 2.78 (q, 2H), 2. 36 (s, 6H), 2.38 (m, 1H), 2.21 (m, 2H), 2.01 (m, 2H), 1.47 (m, 2H), 1.28 (m, 2H), 1.26 (t, 3H).

33 cis 8 8.41 (s, 1H), 5.53 (d, 1H), 4.27 (m, 1H), 2.79 (q, 2H), 2.64 (m, 3H), 2.42 (s, 3H), 2.12-1.47 (m, 10H), 1.34 (m, 2H), 1.26 (t, 3H), 0.95 (t, 3H).

35 cis 8 8.58 (s, 1H), 4.13 (q, 2H), 4.06 (m, 1H), 3.95 (m, 1H), 2.91 (s, 3H), 2.90 (q, 2H), 2.84 (s, 3H), 2.15 (m, 2H), 1.83-1.44 (m, 6H), 1.31 (t, 3H), 1.26 (t, 3H).

36 cis 8 8.41 (s, 1H), 5.46 (d, 1H), 4.22 (m, 1H), 3.55 (s, 3H), 2.78 (q, 2H), 2.59 (s, 3H), 2.51 (m, 1H), 1.93-1.60 (m, 8H), 1. 26 (t, 3H).

39 cis 8 8.43 (s, 1H), 7.24 (m, 2H), 6.82 (d, 2H), 6.74 (t, 1H), 5.58 (br d, 1H), 4.33 (m, 1H), 3.67 (m, 1H), 2.82 (s, 3H), 2.81 (q, 2H), 2.10 (m, 2H), 1.74 (m, 6H), 1.28 (t, 3H).

40 trans 8 8.42 (s, 1H), 7.23 (m, 2H), 6.79 (d, 2H), 6.71 (t, 1H), 5.20 (d, 1H), 3.99 (m, 1H), 3.66 (tt, 1H), 2.79 (s, 3H), 2.78 (q, 2H), 2.23 (d, 2H), 1.94-1.66 (m, 4H), 1.41 (m, 2H), 1.26 (t, 3H).

Cmpd Isomer 1 H NMR Data b No. <BR> <BR> <BR> <BR> <BR> <P> 41 cis 6 8.43 (s, 1H), 7.24 (m, 2H), 6.79 (d, 2H), 6.71 (t, 1H), 5.58 (d, 1H), 4. 34 (m, 1H), 3.63 (m, 1H), 3.30 (q, 2H), 2.82 (q, 2H), 2.08 (br d, 2H), 1.88-1.63 (m, 6H), 1.28 (t, 3H), 1.17 (t, 3H). <BR> <BR> <BR> <BR> <P> 41 trans 8 8.42 (s, 1H), 7.21 (m, 2H), 6.74 (d, 2H), 6.68 (t, 1H), 5.21 (d, 1H), 4.01 (m, 1H), 3.63 (m, 1H), 3.29 (q, 2H), 2.78 (q, 2H), 2.23 (br d, 2H), 1.96 (br d, 2H), 1.65 (m, 2H), 1.40 (m, 2H), 1.27 (t, 3H), 1.17 (t, 3H).

42 cis 8 8.41 (s, 1H), 7.38-7.11 (m, 7H), 6.72 (m, 3H), 5.51 (br d, 1H), 4.50 (s, 2H), 4.32 (m, 1H), 3.88 (m, 1H), 2.78 (q, 2H), 2.08 (br d, 2H), 1.93-1.57 (m, 6H), 1.26 (t, 3H).

43 trans 8 8.38 (s, 1H), 7. 34-7.11 (m, 7H), 6.70 (m, 3H), 5.19 (d, 1H), 4.48 (s, 2H), 3.97 (m, 1H), 3.86 (m, 1H), 2.77 (q, 2H), 2.21 (br d, 2H), 2.00 (br d, 2H), 1.66 (m, 2H), 1.41 (m, 2H), 1.25 (t, 3H).

44 cis 8 8.43 (s, 1H), 7.22 (m, 2H), 6.76 (m, 3H), 5.91 (m, 1H), 5.57 (d, 1H), 5.21 (m, 3H), 4. 33 (m, 1H), 3.87 (m, 2H), 3.73 (m, 1H), 2.80 (q, 2H), 2.09 (brd, 2H), 1.92-1.59 (m, 6H), 1.28 (t, 3H).

45 trans 8 8.41 (s, 1H), 7.21 (dd, 2H), 6.72 (m, 3H), 5.89 (m, 1H), 5.19 (m, 3H), 4.20 (m, 1H), 3.86 (m, 2H), 3.73 (m, 1H), 2.79 (q, 2H), 2.23 (br d, 2H), 1.97 (br d, 2H), 1.67 (m, 2H), 1.41 (m, 2H), 1.26 (t, 3H).

46 cis 8 8.42 (s, 1H), 7.28 (m, 2H), 6.99 (m, 2H), 6.86 (t, 1H), 5.57 (d, 1H), 4.31 (m, 1H), 3.99 (d, 2H), 3.70 (m, 1H), 2.80 (q, 2H), 2.22 (t, 1H), 2.04 (m, 2H), 1.94-1.68 (m, 6H), 1.27 (t, 3H).

49 trans 8 8.40 (s, 1H), 7.25 (dd, 2H), 6.90 (d, 2H), 6.83 (t, 1H), 5. 20 (d, 1H), 3.97 (m, 1H), 3.67 (t, 2H), 3.53 (m, 1H), 3. 37 (t, 2H), 2.78 (q, 2H), 2.23 (br d, 2H), 1.94 (br d, 2H), 1.87-1.58 (m, 3H), 1.38 (m, 2H), 1.26 (t, 3H).

50 cis 8 8.43 (s, 1H), 7.24 (m, 2H), 6.73 (m, 3H), 5.57 (d, 1H), 4.34 (m, 1H), 3.90 (s, 2H), 3.77 (m, 1H), 2.80 (q, 2H), 2.08 (m, 2H), 1.98-1.50 (m, 6H), 1.45 (s, 9H), 1.28 (t, 3H).

54 cis 8 8.36 (s, 1H), 7.44 (m, 3H), 7.22 (m, 2H), 5.27 (d, 1H), 4.67 (tt, 1H), 4.26 (m, 1H), 2.73 (q, 2H), 1.97 (br d, 2H), 1.78 (m, 4H), 1.34 (m, 2H), 1.23 (t, 3H), 1.12 (m, 1H), 0.98 (m, 2H), 0.57 (m, 2H).

58 cis 5 8.37 (s, 1H), 7.43-7.27 (m, 3H), 7.12 (m, 2H), 5. 32 (d, 1H), 4.34-4.06 (m, 4H), 2.74 (q, 2H), 1.99 (br d, 2H), 1.85 (br d, 2H), 1.73 (m, 2H), 1.47 (m, 2H), 1.23 (t, 3H), 1.16 (t, 3H).

61 cis 8 8.37 (s, 1H), 7.41-7.25 (m, 3H), 7.09 (m, 2H), 5.31 (d, 1H), 4. 31-4.11 (m, 2H), 2.73 (q, 2H), 2.04-1.65 (m, 6H), 1.42 (m, 2H), 1.37 (s, 9H), 1.23 (t, 3H).

63 cis 8 8. 38 (s, 1H), 7.34 (m, 2H), 7.19 (m, 1H), 7.06 (m, 2H), 5.53 (d, 1H), 4. 31 (m, 1H), 3.99 (m, 1H), 2.75 (q, 2H), 2.62 (s, 6H), 1.97 (br d, 2H), 1.89-1.61 (m, 6H), 1. 24 (t, 3H).

Cmpd Isomer 1H NMR Data b No.

65 cis 5 8.35 (s, 1H), 7.73 (m, 2H), 7.58-7.29 (m, 6H), 7.05 (m, 2H), 5.12 (d, 1H), 4.28 (tt, 1H), 4.22 (m, 1H), 2.70 (q, 2H), 2.01-1.67 (m, 6H), 1.33 (m, 2H), 1.20 (t, 3H).

66 cis 8 8.42 (s, 1H), 5.61 (d, 1H), 4. 33 (m, 1H), 4.28 (m, 1H), 3.79 (s, 3H), 2.80 (q, 2H), 2.16 (s, 3H), 2.06 (m, 2H), 1.97-1.68 (m, 6H), 1.27 (t, 3H).

71 cis 8 8.42 (s, 1H), 8.38 (s, 1H), 5.41 (d, 1H), 5.31 (d, 1H), 4.47 (s, 2H), 4.20 (m, 2H), 3.83 (s, 3H), 3.49 (s, 3H), 2.80 (q, 2H), 1.95 (m, 4H), 1.75 (m, 4H), 1. 27 (t, 3H).

73 cis 8 8.41 (s, 1H), 5.88 (d, 1H), 5.31 (d, 1H), 4.17 (m, 1H), 3.49 (m, 1H), 2.79 (q, 2H), 1.92 (m, 6H), 1.68 (m, 2H), 1. 36 (s, 9H), 1.27 (t, 3H).

74 cis 8 8.41 (s, 1H), 5.54 (d, 1H), 4. 30 (m, 1H), 2.79 (m, 7H), 2.17-1.42 (m, 14H), 1.26 (t, 3H).

74 trans 8 8.40 (s, 1H), 5.17 (d, 1H), 3.96 (m, 1H), 2.94-2.61 (m, 7H), 2.32-1.28 (m, 14H), 1.25 (t, 3H).

79 cis 8 8.41 (s, 1H), 5.48 (d, 1H), 4.24 (m, 1H), 2.78 (q, 2H), 2.71-2.34 (m, 8H), 2.30 (s, 3H), 2.23 (m, 1H), 1.97-1.53 (m, 8H), 1.26 (t, 3H).

81 cis 8 8.40 (s, 1H), 5.49 (d, 1H), 4.24 (m, 1H), 2.78 (q, 2H), 2.75-2.33 (m, 8H), 2.42 (q, 2H), 2.23 (m, 1H), 1.97-1.52 (m, 8H), 1.26 (t, 3H), 1.10 (t, 3H).

83 cis 8 8.40 (s, 1H), 7.34-7.20 (m, 5H), 5.48 (d, 1H), 4.23 (m, 1H), 3.52 (s, 2H), 2.77 (q, 2H), 2.54 (m, 8H), 2.22 (m, 1H), 1.97-1.52 (m, 8H), 1.26 (t, 3H).

89 cis 8 8.41 (s, 1H), 8.20 (ddd, 1H), 7.48 (ddd, 1H), 6.66 (d, 1H), 6.62 (dd, 1H), 5.49 (d, 1H), 4.25 (m, 1H), 3.56 (m, 4H), 2.78 (q, 2H), 2.67 (m, 4H), 2.29 (m, 1H), 2.01-1.59 (m, 8H), 1. 26 (t, 3H).

90 trans 8 8.41 (s, 1H), 8.20 (m, 1H), 7.47 (m, 1H), 6.63 (m, 2H), 5.19 (d, 1H), 3.96 (m, 1H), 3.55 (m, 4H), 2.78 (q, 2H), 2.70 (m, 4H), 2.41 (t, 1H), 2.22 (d, 2H), 2.01 (d, 2H), 1.51 (q, 2H), 1.28 (m, 2H), 1.26 (t, 3H).

91 cis 8 8.41 (s, 1H), 6.66 (s, 2H), 5.79 (d, 1H), 4.42 (m, 1H), 4.04 (tt, 1H), 2.81 (q, 2H), 2.32 (m, 2H), 2.07 (br d, 2H), 1.67 (m, 4H), 1.28 (t, 3H). b 1H NMR spectra are recorded in CDC13 unless otherwise indicated. 1H NMR spectra are reported in ppm downfield from tetramethylsilane; s = singlet, d = doublet, t = triplet, q = quartet, m = multiplet, dd = doublet of doublets, dt = doublet of triplets, dq = doublet of quartets, ddd = doublet of doublet of doublets, ddt = double of doublet of triplets, tt = triplet of triplets, br s = broad singlet and br d = broad doublet.

BIOLOGICAL EXAMPLES OF THE INVENTION TEST A Fall Armyworm Test units, each consisting of a H. I. S. (high impact styrene) tray with 16 cells were prepared. Wet filter paper and approximately 8 cm2 of lima bean leaf was placed into twelve of the cells. A 0.5-cm layer of wheat germ diet was placed into the four remaining cells.

Fifteen to twenty third-instar larvae of fall armyworm (Spodoptera frugiperda) were placed

into a 230-mL (8-ounce) plastic cup. Solutions of each of the test compounds in 75: 25 acetone-distilled water solvent were sprayed into the tray and cup. Spraying was accomplished by passing the tray and cup on a conveyer belt directly beneath a flat fan hydraulic nozzle which discharged the spray at a rate of 0.138 kilograms of active ingredient per hectare (about 0.13 pounds per acre) at 207 kPa (30 p. s. i.). The insects were transferred from the 230-mL cup to the H. I. S. tray (one insect per cell). The trays were covered and held at 27°C and 50% relative humidity for 48 hours, after which time readings were taken on the twelve cells with lima bean leaves. The four remaining cells were read at 6-8 days for delayed toxicity. Of the compounds tested, the following gave control efficacy levels of 80% or greater: 1,5,10,15,18,26,71,72 and 92.

TEST B Tobacco Budworm The test procedure of TEST A was repeated for determining efficacy against third-instar larvae of the tobacco budworm (Heliothis virescens) except that three 230-mL (8-ounce) plastic cups with wheat germ diet were used in place of the H. I. S. tray, with each cup pre-infested with five third-instar larvae. Of the compounds tested, the following gave mortality levels of 80% or higher: 1,10,18,46,71 and 92.

TEST C Southern Corn Rootworm Test units, each consisting of a 230-mL (8-ounce) plastic cup containing a 6.5-cm2 (1-square-inch) plug of a wheatgerm diet, were prepared. The test units were sprayed as described in TEST A with individual solutions of the test compounds. After the spray on the cups had dried, five second-instar larvae of the southern corn rootworm (Diabrotica undecimpunctata howardi) were placed into each cup. The cups were held at 27°C and 50% relative humidity for 48 hours, after which time mortality readings were taken. The same units were read again at 6-8 days for delayed toxicity. Of the compounds tested, the following gave control efficacy levels of 80% or greater: 1,10,15,18,19,20,21,24,26,27, 31,33,37,39,40,41,42,46,47,48,51,53,58,63,69,71,72,73,75,77 and 92.

TEST D Two-Spotted Spider Mite Pieces of kidney bean leaves, each approximately 6.5 cm2 (1 square inch) in area, that had been infested on the undersides with 25 to 30 adult mites (Tetranychus urticae), were sprayed with their undersides facing up on a hydraulic sprayer with a solution of the test compound in 75: 25 acetone-distilled water solvent. Spraying was accomplished by passing the leaves, on a conveyor belt, directly beneath a flat fan hydraulic nozzle which discharged the spray at a rate of 0.138 kilograms of active ingredient per hectare (about 0.13 pounds per acre) at 207 kPa (30 p. s. i.). The leaf squares were then placed underside-up on a square of wet cotton in a petri dish and the perimeter of the leaf square was tamped down onto the

cotton with forceps so that the mites could not escape onto the untreated leaf surface. The test units were held at 27°C and 50% relative humidity for 48 hours, after which time mortality readings were taken. Of the compounds tested, the following gave mortality levels of 80% or higher: 1,5,6,10,15,18,19,21,22,23,24,25,26,27,33,37,39,40,41,42,44, 61,62,63,68,69,70,71,72,73,74,77 and 92.

TEST E Corn Planthopper Test Test Unit: The test unit consists of a plastic cup containing 126 +/-4 grams of sterilized, non-fertilized sassafras (sandy loam) soil. One pre-germinated Pioneer variety 3394 corn seed is placed in a 1 inch depression in the soil and covered. The test unit is watered with 15 mL of distilled water and placed in a closed Plexiglas box inside a greenhouse operating at 24 degrees centigrade and 36% relative humidity for 4 days at which time it is ready for test. A snug fitting test unit lid with a small opening at the top is placed on all test units prior to test.

Compound Application: Test compounds are formulated at 200 ppm in 20% acetone: 80% water containing 500 ppm Ortho X-77 surfactant. Compounds are applied through the opening in the test unit lid with an atomizer sprayer fitted with a Model 17690-1/8JJAU nozzle and a spray set-up consisting of a J2850 Fluid Cap and J70 Air Cap (Spray Systems, Inc.). The sprayer was operated at 12-13 psi. For each compound, 2 test units are sprayed with a total of 2 mL each of test solution. After spraying, test units are placed in a ventilated enclosure for 10-15 minutes to dry.

Insect Infesting/Evaluation: After drying, a thin layer of white quartz sand is poured onto the soil of each test unit to aid in the evaluation of live and dead insects at the conclusion of the test. Each unit is infested with a minimum of 15 nymphs of the corn planthopper (Peregrinus maidis) which are approximately 21 days old. Infested test units are held in a growth chamber operating at 22 degrees centigrade and 50% relative humidity with a 16: 8 light : dark photoperiod. Insect mortality is evaluated at 6 days post-infestation.

Moribund insects are counted as dead. Of the compounds tested, the following gave mortality of 80% or greater: 1,5,10,15,18,19,21,22,24,26,37,39,46,47,50,58,60, 70,71,72 and 92.

TEST F Green Peach Aphid Test A turnip plant infested with Green Peach Aphid (Myzus persicae) serves as a test unit for this bioassay. All plants have between 15 and 25 aphids (all life stages) on them. The turnip plants are sprayed with a single rate of 0.25 lb. AI/A of each compound at 30 p. s. i. on a moving belt sprayer. All test compounds are formulated using 75/25 acetone/distilled water solvent. All treatments are replicated once. A soil drench of the compound is also applied to each test unit. The drench consists of 2 mL the compound at 0.25 lb. AI/A.

Mortality is assessed at 7 days post compound application by counting live and dead insects under a microscope. Of the compounds tested, the following gave mortality of 80 % or greater: 1,10,18,26,70 and 71.

Test compounds in Tests G-K were first dissolved in acetone in an amount equal to 3% of the final volume and then suspended at a concentration of 200 ppm in purified water containing 250 ppm of the surfactant Trem 014 (polyhydric alcohol esters). The resulting test suspensions were then used in Tests G-K. Spraying these 200 ppm test suspensions to the point of run-off on the test plants is the equivalent of a rate of 500 g/ha.

TEST G The test suspension was sprayed to the point of run-off on wheat seedlings. The following day the seedlings were inoculated with a spore dust of Erysiphe graminis f. sp. tritici, (the causal agent of wheat powdery mildew) and incubated in a growth chamber at 20°C for 7 days, after which disease ratings were made.

TEST H The test suspension was sprayed to the point of run-off on wheat seedlings. The following day the seedlings were inoculated with a spore suspension of Puccinia recondita (the causal agent of wheat leaf rust) and incubated in a saturated atmosphere at 20°C for 24 h, and then moved to a growth chamber at 20°C for 6 days, after which disease ratings were made.

TEST I The test suspension was sprayed to the point of run-off on rice seedlings. The following day the seedlings were inoculated with a spore suspension of Pyricularia oryzae (the causal agent of rice blast) and incubated in a saturated atmosphere at 27°C for 24 h, and then moved to a growth chamber at 30°C for 5 days, after which disease ratings were made.

TEST J The test suspension was sprayed to the point of run-off on tomato seedlings. The following day the seedlings were inoculated with a spore suspension of Phytophthora infestans (the causal agent of potato and tomato late blight) and incubated in a saturated atmosphere at 20°C for 24 h, and then moved to a growth chamber at 20°C for 5 days, after which disease ratings were made.

TEST K The test suspension was sprayed to the point of run-off on cucumber seedlings. The following day the seedlings were inoculated with a spore suspension of Botrytis cinerea (the causal agent of gray mold on many crops) and incubated in a saturated atmosphere at 20°C for 48 h, and moved to a growth chamber at 20°C for 5 days, after which disease ratings were made.

Results for Tests G-K are given in Table A. In the table, a rating of 100 indicates 100% disease control and a rating of 0 indicates no disease control (relative to the controls).

A dash (-) indicates no test results. ND indicates disease control not determined due to phytotoxicity.

TABLE A Cmpd No. Test G Test H Test I Test J Test K 1 99 100 86 99 2 32 86 0 0- 000-30 4 0 0 0 5- 5 0 0 0 21 0 6 0 0 0 0 0 7 0 0 0 63 0 8 0 0 0 85 0 9 0 25 0 76 8 10 100 100 86 ND 43 15 100 100 86-0 18 99 100 0 75 0 19 0 99 0 ND 69 20 39 0 0 61 19 21 95 100 0-0 22 86 0 0 47 65 23 61 0 0 26 0 24 0 0 0 0 0 25 97 99 0 86 0 26 99 100 0 93 0 27 98 99 0 47 0 31 77 85 0 62 8 32 0 0 0 23 8 33 62 97 0 86 8 34 0 25 0 23 47 37 99 100 53 100 47 38 98 0 0 21 0 39 20 100 0 100 48 40 80 97 0 84 0 41 80 94 0 92 0 42 88 86 0 74 94 43 93 0 0 59 83 44 80 86 0 99 0 45 46 68 0 92 0 46 97 100 0 95 0 47 99 100 53 ND 0 Cmpd No. Test G Test H Test I Test J Test K <BR> <BR> <BR> 48 97 97 0 99 0<BR> <BR> <BR> <BR> <BR> 49 96 0 0 74 0 50 86-0 ND 0 <BR> <BR> <BR> 51 97 99 53 0 83<BR> <BR> <BR> <BR> <BR> 52 73 85 0 45 0<BR> <BR> <BR> <BR> <BR> 53 90 0 0 23 94<BR> <BR> <BR> <BR> <BR> 54 87 28 0 0 0<BR> <BR> <BR> <BR> <BR> 55 0 0 0 0 96<BR> <BR> <BR> <BR> <BR> 56 55 27 0 23 0<BR> <BR> <BR> <BR> <BR> 57 90 97 0 0 0<BR> <BR> <BR> <BR> <BR> 58 99 99 0 0 0<BR> <BR> <BR> <BR> <BR> 59 88 0 0 16 0<BR> <BR> <BR> <BR> <BR> 60 95 0 0 ND 0 61 0 0 0 0 0 62 90 85 0 0 94 63 0 0 0 26 65 64 0 0 0 0 0 <BR> <BR> <BR> 65 0 0 0 0 88<BR> <BR> <BR> <BR> <BR> 68 95 99 86 ND 8<BR> <BR> <BR> <BR> <BR> 69 86 93 53 0 8<BR> <BR> <BR> <BR> <BR> 70 61 0 0 26 39<BR> <BR> <BR> <BR> <BR> 71 55 100 53 97 0<BR> <BR> <BR> <BR> <BR> 72 94 99 0 ND 0<BR> <BR> <BR> <BR> <BR> <BR> 73 0 66 0 ND 8<BR> <BR> <BR> <BR> <BR> 74 63 68 0 21 0<BR> <BR> <BR> <BR> <BR> 75 62 85 0 86 8<BR> <BR> <BR> <BR> <BR> 76 0 0 0 45 47<BR> <BR> <BR> <BR> <BR> 77 0 97 0 100 8<BR> <BR> <BR> <BR> <BR> 78 0 0 0 45 8<BR> <BR> <BR> <BR> <BR> 91 0 85 0 ND 69<BR> <BR> <BR> <BR> <BR> 92 95 100 74 26 0<BR> <BR> <BR> <BR> <BR> 93 0 0 0 60 0<BR> <BR> <BR> <BR> <BR> 94 0 0 0 85 0