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1. 发明专利

JPS63174955A PRODUCTION OF N-ALKYLATED AMINO ACID ESTER 失效
公开(公告)号：JPS63174955A
公开(公告)日：1988-07-19
申请号：JP408987
申请日：1987-01-13
申请人： DAICEL CHEM
发明人： SATO KAZUO , GOTO YUKIHISA , YAMAZAKI NORITSUGU , TAKASE ICHIRO
IPC分类号： C07C229/16 , C07C67/00 , C07C227/00 , C07C227/04 , C07C227/08 , C07C227/10 , C07C227/18 , C07C229/24 , C07C229/26 , C07C229/36
摘要： PURPOSE:To obtain a compound useful as various kinds of physiologically active substances and intermediate thereof from readily available raw material in good yield, by reacting a alpha-amino acid ester having a specific molar ratio with a alpha-substituted carboxylic acid ester in the presence of a base. CONSTITUTION:A alpha-amino acid ester is reacted with a alpha-substituted carboxylic acid ester having eliminating group in alpha-position in the presence of a base such as anhydrous sodium carbonate, etc., at 20-120 deg.C for 1-30hr, preferably at 40-90 deg.C. The reaction is carried out using excess amount than equimolar alpha-amino acid ester based on alpha-amino acid ester to provide the aimed product expressed by the formula (R1 and R4 are alkyl, aralkyl, aryl, etc.; R2 and R3 are alkyl, aralkyl, aryl, hetero ring-substituted alkyl, etc.; * is asymmetric carbon).

2. 发明专利

JP2009132620A Phenylthiazole derivative 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：JP2009132620A
公开(公告)日：2009-06-18
申请号：JP2006061344
申请日：2006-03-07
申请人： Astellas Pharma Inc , Daicel Chem Ind Ltd , アステラス製薬株式会社 , ダイセル化学工業株式会社
发明人： KATO TAKESHI , SUZUKI TAKAYUKI , ONDA KENICHI , IMAMURA MASAKAZU , NAKANISHI KEITA , KOIKE TAKANORI , OKUMURA MITSUAKI , ISHIBASHI NAOKI , YOKONO MASANORI , TAKASE ICHIRO , HEIYU TAKAHIRO
IPC分类号： C07D277/28 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P1/02 , A61P1/04 , A61P1/12 , A61P1/14 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P27/00 , A61P27/02 , A61P27/12 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/18 , A61P31/20 , A61P35/00 , A61P35/02 , A61P43/00 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/107 , C07D491/113
CPC分类号： C07D417/12 , C07D277/56 , C07D277/66 , C07D417/06 , C07D417/14 , C07D471/10 , C07D491/08 , C07D491/10
摘要： PROBLEM TO BE SOLVED: To provide a new compound having an activating effect of peroxysome proliferator-activated receptor (PPAR) and especially useful as a therapeutic agent of diabetes.
SOLUTION: This compound is a phenylthiazole derivative expressed by formula (I) [wherein, R
1 is a halogen, an alkyl or the like; (j) is an integer of 0 to 4; X is O or the like; R
2 , R
3 are each H or the like; R
4 is H or a lower alkyl; R
5 is H, a lower alkyl or the like; R
6 is a heterocyclic ring such as piperidine, piperazine or the like; (k) is an integer of 0 to 2; and (n) is an integer of 1 to 5] or its pharmaceutically acceptable salt.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供具有过氧化物酶体增殖物激活受体（PPAR）活化作用的新化合物，特别可用作糖尿病治疗剂。解决方案：该化合物是由式（I）表示的苯基噻唑衍生物[其中R 1是卤素，烷基等; （j）为0〜4的整数。 X是O等; R 2 ，R 3 分别为H等; R 4是H或低级烷基; R 5是H，低级烷基等; R 6是一种杂环，例如哌啶，哌嗪等; （k）为0〜2的整数，和（n）为1〜5的整数]或其药学上可接受的盐。版权所有（C）2009，JPO＆INPIT

3. 发明专利

JPH1059899A PRODUCTION OF ALIPHATIC CARBOXYLIC ACID TERTIARY BUTYL ESTER 失效
公开(公告)号：JPH1059899A
公开(公告)日：1998-03-03
申请号：JP21701096
申请日：1996-08-19
申请人： DAICEL CHEM
发明人： TAKASE ICHIRO , UCHIYAMA ATSUSHI
IPC分类号： C07C67/24 , C07C69/14 , C07C69/24 , C07C69/63
摘要： PROBLEM TO BE SOLVED: To provide a method for producing an aliphatic carboxylic acid tertiary butyl ester, enabling to obtain the desired t-butyl ester only by mixing methyl tertiary butyl ester with target carboxylic acid. SOLUTION: An aliphatic carboxylic acid of formula I (R is an alkyl, a halogenated alkyl) is reacted with methyl tertiary butyl ether(MTBE) to obtain an aliphatic carboxylic acid tertiary butyl ester of formula II. The MTBE is preferably used in an amount of >=1 mole, preferably several ten-fold moles to several hundred-fold moles, that of the carboxylic acid. The reaction is preferably carried out in a temperature range from room temperature to the refluxing temperature of MTBE. The objective compound can thereby simply be obtained.

4. 发明专利

JP2523825B2 失效
公开(公告)号：JP2523825B2
公开(公告)日：1996-08-14
申请号：JP25302088
申请日：1988-10-07
申请人： DAICEL CHEM
发明人： MATSUYAMA AKIKAZU , TAKASE ICHIRO , UEDA YOICHIRO , KOBAYASHI YOSHINORI
IPC分类号： C12P7/42 , C12R1/01 , C12R1/025 , C12R1/06 , C12R1/07 , C12R1/13 , C12R1/15 , C12R1/20 , C12R1/22 , C12R1/37 , C12R1/38 , C12R1/64 , C12R1/645 , C12R1/72 , C12R1/78

5. 发明专利

JPH05306265A 失效
公开(公告)号：JPH05306265A
公开(公告)日：1993-11-19
申请号：JP13156892
申请日：1992-04-24
申请人： DAICEL CHEM
发明人： TAKASE ICHIRO
IPC分类号： B01J31/12 , C07B61/00 , C07C303/30 , C07C305/26 , C07C309/65 , C07C309/73
摘要： PURPOSE:To produce the subject compound useful as an intermediate for synthesis of a medicine such as an antibiotics by reacting an alpha-sulfonyloxycarboxylic acid ester with an alcohol in a specified molar ratio in the presence of a titanic acid ester catalyst. CONSTITUTION:The subject compound of formula II is obtained by carrying out an ester interchange reaction between a compound of formula I (R is a 1 to 6C alkyl, an aryl or an aralkyl; R is a halogen, a lower alkyl, a halogenated lower alkyl or an aryl; R is a 1 to 4C alkyl or a 2 to 4C alkenyl) and a compound of formula R OH (R is a 2 to 10C alkyl, a 2-substituted ethyl, a cycloalkyl, etc.) in the presence of a titanic acid ester catalyst (e.g. tetraisopropyl titanate) in a solvent (e.g. toluene) at 70 to 150 deg.C. In this reaction, the alcohol and the catalyst are used respectively in an amount of 1.0 to 1.4mol and 0.01 to 20mol based on 1mol the compound of formula I. The subject compound can be obtained from readily available raw materials in a high yield with a simple operation.

6. 发明专利

JPH0374346A PREPARATION OF 2-OXO-4-PHENYLBUTANOIC ACID DERIVATIVE 失效
公开(公告)号：JPH0374346A
公开(公告)日：1991-03-28
申请号：JP20838789
申请日：1989-08-11
申请人： DAICEL CHEM
发明人： TAKASE ICHIRO , UEDA YOICHIRO
IPC分类号： C07C51/36 , B01J23/44 , C07B61/00 , C07C59/84
摘要： PURPOSE:To prepare the subject compound useful as an intermediate for synthesizing drugs or various amino acids, etc., by setting a pH of the solution of a 2-oxo-4-phenyl-3-butenoic acid derivative in a specified range and subsequently catalytically reducing the derivative in the presence of a Pd catalyst. CONSTITUTION:A 2-oxo-4-phenyl-3-butenoic acid derivative of formula I (M is H, alkali metal or alkaline earth metal) is reduced in the presence of a palladium catalyst in a solution set to a pH of 6-10.5 to provide a 2-oxo-4- phenylbutanoic acid derivative of formula II. The reaction is especially preferably performed in a slurry state and is a profitable method.

7. 发明专利

JPH0223876A PRODUCTION OF (R)-2-HYDROXY-4-PHENYL-3-BUTENOIC ACID 失效
公开(公告)号：JPH0223876A
公开(公告)日：1990-01-26
申请号：JP17347088
申请日：1988-07-12
申请人： DAICEL CHEM
发明人： MATSUYAMA AKIKAZU , TAKASE ICHIRO , UEDA YOICHIRO , KOBAYASHI YOSHINORI
IPC分类号： C12P7/42 , C12R1/01 , C12R1/225 , C12R1/46
摘要： PURPOSE:To obtain the subject butenoic acid having high optical purity and useful as pharmaceuticals, etc., by the asymmetric reduction of a specific butenoic acid with microorganism of genus Lactobacillus, Leuconostoc, etc. CONSTITUTION:The objective butenoic acid is produced by treating 2-keto-4- phenyl-3-butenoic acid with a microbial strain selected from a microbial group belonging to genus Lactobacillus, Leuconostoc, Streptococcus, Pediococcus and Sporolactobacillus and having asymmetric reduction capability or with a treated material of the microorganism.

8. 发明专利

JPS63183543A PRODUCTION OF ALPHA-HYDROXYKETONES 失效
公开(公告)号：JPS63183543A
公开(公告)日：1988-07-28
申请号：JP17971387
申请日：1987-07-17
申请人： DAICEL CHEM
发明人： SATO KAZUO , YAMAZAKI NORITSUGU , TAKASE ICHIRO
IPC分类号： C07C45/67 , C07B61/00 , C07C45/00 , C07C45/51 , C07C45/54 , C07C49/17 , C07C49/245 , C07C49/747 , C07C49/83 , C07C67/00
摘要： PURPOSE:To safely and advantageously obtain the titled compound which is an intermediate of medicine and agricultural chemicals in high yield, by dispersing a specific compound such as alpha-hydroxyisobutylphenone or the like using an aqueous alkali solution and heat-reacting the compound, when the titled compound is obtained from the above-mentiond specific compound. CONSTITUTION:A compound (e.g. alpha-chloroisobutylophenone, 2-hydroxy-3-oxo-2,4- dimethylpentane, etc.) expressed by formula I (R1 and R3 are alkyl, alkenyl or aryl; R2 is H, alkyl, alkenyl or aryl; X is hydroxy or halogen) is dispersed in an aqueous alkali solution and heat-reacted at the boiling point of water or below to provide the compound expressed by formula II. The alkaline substance is used in an amount of 0.02-50mol. when X is hydroxyl group and 1.02-50mol. When X is halogen based on the compound expressed by formula I and an alkali concentration in aqueous alkali solution is preferably 0.5-8 N. The reaction system is preferably stirred.

9. 发明专利

JPS63170344A N-ALKYLATION OF AMINO ACID ESTER 失效
公开(公告)号：JPS63170344A
公开(公告)日：1988-07-14
申请号：JP279087
申请日：1987-01-09
申请人： DAICEL CHEM
发明人： TAKASE ICHIRO , SATO KAZUO , GOTO YUKIHISA , YAMAZAKI NORITSUGU
IPC分类号： C07B53/00 , C07B31/00 , C07B43/04 , C07C67/00 , C07C227/00 , C07C227/08 , C07C227/18 , C07C229/16 , C07C229/26 , C07C229/36 , C07C271/08 , C07C279/14 , C07D233/64
摘要： PURPOSE:To obtain a compound useful as various performed chemical mediators or an intermediate thereof in high yield without using an expensive and slightly obtainable reagent, by reacting an alpha-amino acid ester with an alpha-substituted carboxylic acid ester. CONSTITUTION:A compound shown by formula I and a compound shown by formula II (R1-R4 are alkyl, aralkyl, cycloalkyl, aryl, etc.; * is asymmetric carbon; X is halogen, aliphatic substituted sulfonyloxy, etc.) or a compound shown by formula III and a compound shown by formula IV are reacted in the presence or absence of a base (e.g. triethylamine) in a solvent (e.g. acetonitrile) or in a solventless state at 20-120 deg.C to give the aimed compound shown by formula V. The amount of the compound shown by the formula I or formula III used is more than equimolar amount of the compound shown by the formula II or formula IV and an amount to make sum of the former and the base larger than twice the molar amount of the latter. The aimed substance is useful as a common intermediate for synthesizing various amino acid derivatives useful as a hypotensor by inhibitory actions on an enzyme capable of converting angiotensin.

10. 发明专利

JPS6330444A DIRECT OPTICAL RESOLUTION OF ACETOIN DERIVATIVE 失效
公开(公告)号：JPS6330444A
公开(公告)日：1988-02-09
申请号：JP17488586
申请日：1986-07-25
申请人： DAICEL CHEM
发明人： ICHIDA AKITO , YAMAZAKI NORITSUGU , TAKASE ICHIRO
IPC分类号： C07B57/00 , C07B31/00 , C07B63/00 , C07C45/00 , C07C45/78 , C07C45/79 , C07C49/17 , C07C49/245 , C07C67/00
摘要： PURPOSE:To make it possible to readily and accurately carry out analysis of optical purity, by optically resolving enantiomers of an acetoin derivative using a separating agent containing a polysaccharide derivative as an active ingredient. CONSTITUTION:Enantiomers of an acetoin derivative utilized as an intermediate for medicines, e.g. 5-methyl-5-phenyl-4,5-dihydro-oxofuran-2-carboxylic acid, etc., which is one of hypolipemic factors, synthesized from a ketone derivative an a metal acetylide and expressed by the formula [R is alkyl or (substituted) aromatic group; mark* indicates asymmetric carbon atom] are directly and optically resolved by optical resolution using silica gel, containing a polysaccharide derivative, e.g. cellulose tribenzoate treated with diphenylsilane, etc., as an active ingredient in an optically active stationary phase by liquid chromatography, etc. The polysaccharide of the above-mentioned resolving agent is a synthetic, natural and modified natural polysaccharide and preferably held by a carrier, e.g. cellulose, amylose, etc., capable of readily providing high-purity polysaccharide.

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