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JP2013530209A |
Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially...
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JP5247699B2 |
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JP5236627B2 |
The invention makes it possible to produce, industrially and easily, optically active compounds for constructing substituents in the production of extremely safe quinolone- carboxylic acids having high antibacterial activity. Intermediat...
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JP5236743B2 |
The invention relates to a novel process for preparing enantiomerically enriched or pure tetrahydroquinoline derivatives by reacting a chiral dihydropyran-methylamine C with a aldehyde B and an aniline A in a multicomponent one pot synth...
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JP2013136573A |
To provide a method for efficiently producing optically-active 1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane in a high yield from otpically-active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol while maintaining high optical purity, and fu...
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JP5235018B2 |
This invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the formula wh...
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JP5233299B2 |
There is disclosed a purification method of an optically active 1-(2-trifluoromethylphenyl)ethanol represented by the formula [1], which includes recrystallizing the optically active 1-(2-trifluoromethylphenyl)ethanol from an aliphatic h...
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JP2013129642A |
To easily obtain an optically active 3,4-bis(alkyloxycarbonyl)-1,6-hexanedioic acid derivative in high efficiency.An optically active 3,4-bis(alkyloxycarbonyl)-1,6-hexanedioic acid derivative is produced by precipitating, from a solvent ...
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JP5228166B2 |
The present application relates to novel difluorophenol derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxi...
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JP5212953B2 |
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JP5212740B2 |
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JP2013522273A |
A process for preparing [(1 R ,2 R )-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) ...
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JP5207518B2 |
A new process for preparation of 3-(2-hydroxy-5-methylphenyl)-N,N-diisopropyl-3-phenylpropyla
mine from 3,4-dihydro-6-methyl-4-phenyl-2-benzopyran-2-one is characterized by intermediates such as 3-(2-hydroxy-5-methylphenyl)-3-phenylpropa...
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JP5202519B2 |
This invention relates to the preparation of (R)-(-)-3-(carbamoylmethyl)-5-methylhexanoic acid, in particular, the resolution of the acid racemate by means of salification with optically active amines and subsequent acidification to give...
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JP5200245B2 |
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JP2013095725A |
To provide a method for producing one enantiomer selectively from the racemates of a compound exhibiting a high controlling effect on plant diseases.This method for producing one enantiomer includes reacting an optically active camphor s...
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JP5191385B2 |
The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic aci...
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JP5185127B2 |
The present invention relates to a process for the preparation of optically pure amlodipine gentisate, more particularly to a continuous process for the preparation of optically pure amlodipine gentisate with good yield and high optical ...
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JP5182615B2 |
To provide a method for producing an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid, a basic amino acid salt thereof or an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester with high yield and high optical pu...
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JP5176452B2 |
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JP2013056848A |
To provide a new method for producing an optically active alcohol compound.The method for producing the optically active alcohol compound comprises a step of conducting a reaction of a racemic alcohol compound in the presence of oxygen-c...
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JP5164841B2 |
The invention relates to compounds having general formula (I), wherein R is as defined herein. The invention also relates to acid addition salt, a hydrate or a solvate of compounds of formula (I). The invention further relates to the met...
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JP5153631B2 |
The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily produc...
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JP5149238B2 |
A processes which is industrially advantageous in producing antibacterial agents. An industrially advantageous process for producing an intermediate useful in producing antibactrial agents is provided by producing compound (VI-a) in acco...
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JP2013505215A |
The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use i...
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JP2013032380A |
To provide a simpler preparation method for an enantiomerically and essentially pure compound like levocetirizine or the like by using a novel and enantiomerically and essentially pure intermediate.There is provided a (S)-2-[4-(4-chlorob...
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JP5137284B2 |
The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-su
lfonamide- 7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(...
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JP5124281B2 |
The present invention relates to a method for optical resolution of amlodipines by using isopropanol solvent and optically active O,O′-dibenzoyl tartaric acid as chiral reagent. More particularly, the present invention relates to a met...
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JP5117784B2 |
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JP5122871B2 |
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JP5112074B2 |
The invention is directed at a new process for the preparation of pure enantiomers from the racemate of amidoacetonitrile compounds of formula wherein R1, R2 and R3, independently of each other, signify hydrogen, halogen, nitro, cyano, C...
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JP5112658B2 |
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JP5113978B2 |
As novel salts of monatin, salts with organic amines such as amino acids, aminoalcohols, dipeptide esters, etc. are provided. The salts with amino acids or dipeptide esters can be used as sweeteningmaterials, of which the crystals are st...
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JP5111849B2 |
Process for industrial synthesis of (2S) indoline-2-carboxylic acid (I) by reacting racemic acid (III) with chiral amine to form salts (IV), separating crystals of (2S) salt from (2R) salt and then: (1) acidifying (2S) salt of (IV) to gi...
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JP5113210B2 |
The invention is directed to a process for producing intermediates of a compound which exhibits an activated blood coagulation factor Xa inhibitory action and which is a useful preventive and a therapeutic agent for thrombotic diseases. ...
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JP5107382B2 |
Preparing tetrahydro-benzo[d]azepin-2-one compounds (A) comprises: reacting 3-(7,8-dimethoxy-2-oxo-1,2,4,5-tetrahydro-benzo[d]azepin-3-y
l)-propionitrile (VIII) with (3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-trien-7-ylmethyl)
-methyl-am...
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JP5107381B2 |
Preparing 3-{3-[(3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-trien-7-ylm
ethyl)-methyl-amino]-propyl}-7,8-dimethoxy-1,3,4,5-tetrahydr
o-benzo[d]azepin-2-one (VIII) comprises: reacting 3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-triene-7-carb...
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JP5097559B2 |
Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resoluti...
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JP2012240982A |
To provide an easy and environmentally friendly method for producing a benzenesulfonate of optically active 4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic
acid.The method for producing a benzenesulfonate of optically activ...
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JP2012236799A |
To provide a method for economically producing 1-menthyl (3R)-3-hydroxybutanoate in higher enantiomeric excess at a lower cost.The 1-menthyl (3R)-3-hydroxybutanoate can economically be produced in the higher enantiomeric excess at a lowe...
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JP5092743B2 |
[Problems] To provide a method for efficiently separating and collecting an optically active amino acid amide and an optically active amino acid which are highly important substances as intermediates in the production of various industri...
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JP5092289B2 |
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JP2012530116A |
A process for producing bortezomib N-(pyrazin-2-yl)carbonyl-L-phenylalanine-L-leucine boronic acid) comprising the step of deprotecting the compound of formula XII: to yield bortezomib.
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JP2012530115A |
The present invention is generally related to the field of organic chemistry, especially to the preparation of α-aminoboronic acid derivatives.
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JP5079459B2 |
The invention relates to substantially photochemically cross-linked polysaccharide derivatives that do not contain photopolymerisable functional groups prior to the cross-linking, which can be used as carrier materials for the chromatogr...
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JP5070596B2 |
Provided is a chitosan derivative having a high optical resolving power. Specifically provided is a chitosan derivative represented by the following Formula (I). wherein R 1 represents an aliphatic group or an aromatic group having a car...
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JP2012528181A |
Provided herein are improved processes for the synthesis of substituted tetrahydro beta-carboline derivatives. In particular, provided herein are improved processes useful for the preparation of (S)-4-chlorophenyl 6-chloro-1-(4-methoxyph...
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JP5066638B2 |
The invention relates to N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-c
arboxamidine and its optically active enantiomers. (R)-(-)-N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-o
xide-3-carboxamidine and (S)-(+)-N-[2-h...
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JP5064436B2 |
The invention relates to a process for the preparation of racemic citalopram free base or an acid addition salt thereof and/or R- or S-citalopram as the free base or an acid addition salt thereof by separation of a mixture of R- and S-ci...
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JP5054532B2 |
The present invention relates to compounds having the general formula (I) with the definitions of R 1 -R 6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds as a medicament, prefe...
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