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1. 发明授权

EP0969000B1 Process for reducing alpha-amino ketones 失效
标题翻译：一种用于α-氨基酮的制备方法
公开(公告)号：EP0969000B1
公开(公告)日：2002-12-04
申请号：EP98923095.8
申请日：1998-06-03
申请人： KANEKA CORPORATION
发明人： MATSUO, Kazuhiko , MATSUMOTO, Shingo , INOUE, Kenji
IPC分类号： C07C269/06 , C07C271/16 , C07C323/44 , C07C271/22 , C07B41/02
CPC分类号： C07C269/06 , C07C271/16 , C07C271/22

2. 发明授权

EP0930292B1 PROCESS FOR PREPARING BETA-AMINO-ALPHA-HYDROXY ACID DERIVATIVES 失效
标题翻译： PROCESS FORβ-氨基α-羟基衍生物的制备
公开(公告)号：EP0930292B1
公开(公告)日：2002-10-16
申请号：EP97935797.7
申请日：1997-08-18
申请人： KANEKA CORPORATION
发明人： MATSUMOTO, Shingo , MATSUO, Kazuhiko , SUGAWA, Tadashi , MOROSHIMA, Tadashi , INOUE, Kenji
IPC分类号： C07C229/22 , C07C229/34 , C07C227/02 , C07D209/48 , C07C311/19 , C07D209/26
CPC分类号： C07C303/44 , C07C227/02 , C07C227/42 , C07C269/08 , C07C271/18 , C07C303/40 , C07D209/26 , Y02P20/55 , C07C311/19 , C07C229/22 , C07C229/34
摘要： A process for preparing β-amino-α-hydroxy acid derivatives in an efficient and commercially useable manner. The process is characterized by hydrolyzing an α-amino-α',α'-dihaloketone derivative represented by general formula (1) in the presence of a base, optionally followed by the protection of the amino group, to prepare a β-amino-α-hydroxy acid derivative represented by general formula (2).

3. 发明授权

EP0779366B1 PROCESS FOR PRODUCING OPTICALLY ACTIVE 1-HALO-3-AMINO-4-PHENYL-2-BUTANOL DERIVATIVES 失效
标题翻译： PROCESS FOR PRODUCTION光学活性的1-卤代-3-氨基-4-苯基-2-丁醇衍生物的
公开(公告)号：EP0779366B1
公开(公告)日：2002-04-03
申请号：EP96918833.3
申请日：1996-06-19
申请人： KANEKA CORPORATION
发明人： SUGAWA, Tadashi , INOUE, Kenji
IPC分类号： C12P41/00 , C12P13/02 , C12P13/00
CPC分类号： C12P13/001 , Y10S435/822 , Y10S435/911
摘要： A process for producing optically active 1-halo-3-amino-4-phenyl-2-butanol derivatives from optically active 1-halo-3-amino-4-phenyl-2-butanone derivatives stereoselectively in a high yield by bringing the butanone derivatives into contact with microorganisms.

4. 发明授权

EP0754669B1 PROCESSES FOR PRODUCING ALPHA-HALO KETONES, ALPHA-HALOHYDRINS AND EPOXIDES 失效
标题翻译：用于生产ALPHA卤代酮，α-卤代醇和环氧化物
公开(公告)号：EP0754669B1
公开(公告)日：2001-10-31
申请号：EP96901520.5
申请日：1996-02-02
申请人： KANEKA CORPORATION
发明人： NISHIYAMA, Akira , SUGAWA, Tadashi , MANABE, Hajime , INOUE, Kenji , YOSHIDA, Noritaka
IPC分类号： C07C45/48 , C07C49/80 , C07C29/143 , C07C33/46 , C07C221/00 , C07C225/16 , C07C213/00 , C07C215/28 , C07D301/26 , C07D303/04 , C07C269/06
CPC分类号： C07D303/36 , C07C29/143 , C07C45/48 , C07C269/06 , C07C319/20 , C07C323/43 , C07C31/34 , C07C33/46

5. 发明公开

EP1055671A1 PROCESS FOR PRODUCING SIMVASTATIN 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES SIMVASTATIN PRECURSORS
公开(公告)号：EP1055671A1
公开(公告)日：2000-11-29
申请号：EP99959738.8
申请日：1999-12-10
申请人： KANEKA CORPORATION
发明人： TAOKA, Naoaki , INOUE, Kenji
IPC分类号： C07D309/30 , C07D319/06
CPC分类号： C07D319/06 , C07D309/30 , Y02P20/55
摘要： This invention provides an easy and efficient process for producing a simvastatin of great use as an HMG-CoA reductase inhibitor,

which comprises deacylation of lovastatin with an inorganic base and a secondary or tertiary alcohol and subjecting the resulting did lactone to selective protection with a ketal or acetal protective group, acylation and deprotection-lactonization to give simvastatin.
摘要翻译：本发明提供了一种用于生产作为HMG-CoA还原酶抑制剂的伟大用途的辛伐他汀的简单和有效的方法，其包括用无机碱和仲或叔醇脱氢洛伐他汀，并使所得内酯用缩酮进行选择性保护或缩醛保护基，酰化和去保护 - 内酯化得到辛伐他汀。

6. 发明授权

EP1439162B1 PROCESS FOR PRODUCING OPTICALLY ACTIVE 3,5-DIHYDROXYCARBOXYLIC ACID DERIVATIVE 有权
标题翻译：生产光学活性3,5-二羟基羧酸衍生物的方法
公开(公告)号：EP1439162B1
公开(公告)日：2008-03-26
申请号：EP02777941.2
申请日：2002-10-24
申请人： KANEKA CORPORATION
发明人： SUGAWARA, Masanobu , INOUE, Kenji
IPC分类号： C07C69/675 , C07C69/78 , C07C67/31
CPC分类号： C07C67/31 , C07B2200/07 , C07C67/29 , C07C69/78 , C07C69/675
摘要： A process for producing an optically active 3,5-dihydroxyhexanoic acid derivative by stereoselectively reducing an optically active 3-oxo-5-hydroxyhexanoic acid derivative. It necessitates neither an ultralow-temperature reactor nor an incubator and is a simple and economical process in which protection of the 5-position hydroxy is unnecessary. Hydrogen, which is extremely inexpensive, is used as a reducing agent to asymmetrically hydrogenate an optically active 3-oxo-5-hydroxyhexanoic acid derivative by the catalytic action of a ruthenium/optically active phosphine complex, especially an RuBr2BINAP complex prepared from 2,2'-bisdiarylphosphino-1,1'-binaphthyl (BINAP) and a ruthenium complex, to thereby produce an optically active 3,5-dihydroxyhexanoic acid derivative.
摘要翻译：通过立体选择性还原光学活性的3-氧代-5-羟基己酸衍生物来制备光学活性3,5-二羟基己酸衍生物的方法。它既不需要超低温反应器也不需要培养箱，并且是不需要保护5位羟基的简单且经济的过程。使用非常便宜的氢作为还原剂，通过钌/旋光活性膦配合物的催化作用，使光学活性的3-氧代-5-羟基己酸衍生物不对称地氢化，特别是由2,2-二甲基-1,3-二氧戊环制备的RuBr2BINAP配合物双 - 二芳基膦基-1,1'-联萘（BINAP）和钌配合物，由此制备光学活性的3,5-二羟基己酸衍生物。

7. 发明授权

EP1288213B1 PROCESS FOR PREPARING OPTICALLY ACTIVE 2- 6-(HYDROXY-METHYL)-1,3-DIOXAN-4-YL|ACETIC ACID DERIVATIVES 有权
标题翻译：用于生产光学活性的2-¬6-（羟甲基）-1,3-二恶烷-4-基| ACETIC衍生物（〇一年十二月十九日）
公开(公告)号：EP1288213B1
公开(公告)日：2006-11-29
申请号：EP01936850.5
申请日：2001-06-05
申请人： KANEKA CORPORATION
发明人： NISHIYAMA, Akira , HORIKAWA, Miho , YASOHARA, Yoshihiko , UEYAMA, Noboru , INOUE, Kenji
IPC分类号： C07D319/06 , C07C69/675 , C07C69/716 , C12P7/42
CPC分类号： C07D319/06 , C12P7/42 , C12P17/06
摘要： A process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an enolate prepared by reacting an acetic acid ester derivative with a base or a zero-valent metal with (S)-β-hydroxy-η-butyrolactone at a temperature of -30°C or above to thereby obtain a dihydroxyoxohexanoic acid derivative, treating this derivative with an acylating agent in the presence of a base to thereby obtain a monoacylated derivative of dihydroxyoxohexanoic acid, reducing the monoacylated derivative with a microorganism into a monoacylated derivative of trihydroxyhexanoic acid, treating the resulting derivative with an acetal-forming reactant in the presence of an acid catalyst to thereby obtain an acyloxymethyldioxanylacetic acid derivative, and subjecting this derivative to solvolysis in the presence of a base.

8. 发明授权

EP1078919B1 SYNTHESIS OF ALPHA-AMINO-ALPHA',ALPHA'-DIHALOKETONES AND PROCESS FOR THE PREPARATION OF BETA)-AMINO ACID DERIVATIVES BY THE USE OF THE SAME 有权
标题翻译： α-氨基的ALPHA“阿尔法” DIHALOKETONEN AND PROCESS用于生产BETA） - 氨基酸衍生物通过使用相同的合成
公开(公告)号：EP1078919B1
公开(公告)日：2005-12-07
申请号：EP00907964.1
申请日：2000-03-09
申请人： KANEKA CORPORATION
发明人： NISHIYAMA, Akira , INOUE, Kenji
IPC分类号： C07C269/06 , C07C271/18 , C07C271/22
CPC分类号： C07C269/06 , C07C271/18 , C07C271/22

9. 发明授权

EP1024139B1 PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2-(6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL) ACETIC ACID DERIVATIVES 有权
标题翻译：用于生产光学活性的2-（6-（羟甲基）-1,3-二恶烷-4-基） - 衍生物
公开(公告)号：EP1024139B1
公开(公告)日：2004-05-12
申请号：EP99935066.3
申请日：1999-08-05
申请人： KANEKA CORPORATION
发明人： KIZAKI, Noriyuki , YAMADA, Yukio , YASOHARA, Yoshihiko , NISHIYAMA, Akira , MIYAZAKI, Makoto , MITSUDA, Masaru , KONDO, Takeshi , UEYAMA, Noboru , INOUE, Kenji
IPC分类号： C07D319/06 , C07C67/343 , C07C67/31
CPC分类号： C07D319/06 , C07B2200/07 , C07C67/343 , C07C253/30 , C12P7/62 , C07C69/716 , C07C255/21

10. 发明授权

EP1046634B1 PROCESSES FOR PRODUCING BETA-HALOGENO-ALPHA-AMINO-CARBOXYLIC ACIDS AND PHENYLCYSTEINE DERIVATIVES AND INTERMEDIATES THEREOF 有权
标题翻译：工艺为BETA卤素的α-氨基羧酸，PHENYLCYSTEINDERIVATEN及其中间体的制备
公开(公告)号：EP1046634B1
公开(公告)日：2003-09-10
申请号：EP98961624.8
申请日：1998-12-28
申请人： KANEKA CORPORATION
发明人： YAMASHITA, Koki , INOUE, Kenji , KINOSHITA, Koichi , UEDA, Yasuyoshi , MURAO, Hiroshi
IPC分类号： C07C229/20 , C07C227/16 , C07C227/40 , C07C323/58 , C07C319/14 , C07B53/00
CPC分类号： C07C227/16 , C07C319/14 , Y02P20/55 , C07C323/58 , C07C323/59 , C07C229/20
摘要： An industrially advantageous process for producing β-halogeno-α-aminocarboxylic acids; and a process for producing optically active N-protected-S-phenylcysteine having a high optical purity and its intermediates with the use of the former process. The process for producing β-halogeno-α-aminocarboxylic acids or salts thereof comprises treating with a halogenating agent a β-hydroxy-α-aminocarboxylic acid (wherein the basicity of the amino group at the α-position is not shielded by the presence of the substituent of the amino group) or a salt thereof with an acid to thereby halogenate the hydroxyl group. The process for producing optically active N-protected-S-phenylcysteine represented by general formula (3) or its salt comprises subjecting optically active serine or its salt to the above-mentioned production process and then treating the product with an amino-protective agent followed by a reaction with thiophenol under basic conditions.

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