公开(公告)号：EP1600438A4

公开(公告)日：2007-05-02

申请号：EP04714501

申请日：2004-02-25

申请人： KANEKA CORP

发明人： YAMAMOTO SHOGO ,  TAKEDA TOSHIHIRO ,  FUSE YOSHIHIDE ,  UEDA YASUYOSHI

IPC分类号： C07C319/14 ,  C07B53/00 ,  C07B55/00 ,  C07C51/363 ,  C07C51/43 ,  C07C57/58 ,  C07C319/28 ,  C07C323/56

CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C51/363 ,  C07C319/14 ,  C07C57/58 ,  C07C323/56

摘要： Optically active compounds having thio groups at the 2-position which are important to the production of drugs and so on can be produced with minimized racemization in high yield and at a low cost by chlorinating an optically active compound having a hydroxyl group at the 2-position with the inversion of configuration at the 2-position to form an optically active compound having a chlorine atom at the 2-position, and reacting the optically active compound having a chlorine atom at the 2-position with a metal thiolate to introduce a thio group to the compound with the invention of configuration at the 2-position. Further, optically active compounds having thio groups at the 2-position can be produced at higher optical purities and in higher yields by conducting the reaction of an optically active compound having a chlorine atom at the 2-position with a metal thiolate in the presence of water. Additionally, optically active carboxylic acids having thio groups at the 2-position can be efficiently rid of coexistent impurities such as optical isomers by crystallization in the presence of an aliphatic hydrocarbon solvent and/or a sulfur-containing solvent, whereby optically active carboxylic acids having thio groups at the 2-position can be obtained as crystalline substances at further enhanced purities.

公开(公告)号：EP1179530A4

公开(公告)日：2005-07-27

申请号：EP01904517

申请日：2001-02-16

申请人： KANEKA CORP

发明人： SUGAWARA MASANOBU ,  FUJII AKIO ,  OKURO KAZUMI ,  SAKA YASUHIRO ,  NAGASHIMA NOBUO ,  INOUE KENJI ,  TAKEDA TOSHIHIRO ,  KINOSHITA KOICHI ,  MOROSHIMA TADASHI ,  FUSE YOSHIHIDE ,  UEDA YASUYOSHI

IPC分类号： C07C227/10 ,  C07C227/32 ,  C07C227/42 ,  C07C229/26 ,  C07C229/30 ,  C07C303/36 ,  C07C311/19 ,  C07D203/08 ,  C07D203/20 ,  C07D203/24 ,  C07B53/00 ,  C07C227/04

CPC分类号： C07D203/08 ,  C07B2200/07 ,  C07C227/10 ,  C07C227/32 ,  C07C227/42 ,  C07C229/30 ,  C07C303/36 ,  C07D203/20 ,  C07D203/24 ,  C07C311/19 ,  C07C229/26

摘要： An optically active amino acid derivative is prepared either by subjecting an optically active 3-haloalanine derivative (1) to N-protection followed by cyclization or cyclization followed by N-protection to prepare an optically active aziridinecarboxylic acid derivative (3) whose imino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (3) with an organometallic reagent or by subjecting an optically active 3-haloalanine derivative to N-protection to obtain an optically active 3-haloalanine derivative (4) whose amino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (4) with an organometallic reagent. According to such processes, natural and nonnatural optically active amino acids can be prepared from inexpensive raw materials through simple and easy operation. In said derivatives, X is halogen; R?1 and R2¿ are each hydrogen or the like; * represents an asymmetric carbon atom; and P1 is 2- and/ or 4- nitrated benzenesulfonyl.

公开(公告)号：EP1422215A4

公开(公告)日：2005-07-06

申请号：EP02755871

申请日：2002-08-08

申请人： KANEKA CORP

发明人： YAMASHITA KOKI ,  TAKEDA TOSHIHIRO ,  KINOSHITA KOICHI ,  UEDA YASUYOSHI

IPC分类号： C07C51/363 ,  C07C51/43 ,  C07C51/48 ,  C07C57/58 ,  C07C67/52 ,  C07C67/58 ,  C07C303/28 ,  C07C303/30 ,  C07C309/66 ,  C07B55/00 ,  C07C53/19 ,  C07C67/08 ,  C07C69/675 ,  C07C69/732 ,  C07C309/70

CPC分类号： C07C303/30 ,  C07B2200/07 ,  C07C51/363 ,  C07C51/43 ,  C07C51/48 ,  C07C57/58 ,  C07C67/52 ,  C07C67/58 ,  C07C303/28 ,  Y02P20/55 ,  C07C69/732 ,  C07C309/66

摘要： A process for efficiently producing an optically active 2-bromocarboxylic acid and optically active 2-sulfonyloxycarboxylic acid which are important for producing medicines, etc. An optically active 2-sulfonyloxycarboxylic ester is subjected to protective-group elimination under acid conditions to obtain an optically active 2-sulfonyloxycarboxylic acid. A metal bromide is caused to act on the acid to brominate it with inversion of configuration at the 2-position to thereby produce an optically active 2-bromocarboxylic acid. The resultant optically active 2-bromocarboxylic acid is isolated/purified by subjecting it to a step in which the acid is crystallized and separated as a salt with a base. Thus, an optically active 2-bromocarboxylic acid having a high chemical purity and high optical purity can be produced.

公开(公告)号：EP1988073A4

公开(公告)日：2011-08-24

申请号：EP07706812

申请日：2007-01-16

申请人： KANEKA CORP

发明人： KISHIMOTO NARUMI ,  YASUKOUCHI HIROAKI ,  TAKEDA TOSHIHIRO

IPC分类号： C07C231/14 ,  C07C231/16 ,  C07C231/24 ,  C07C237/04

CPC分类号： C07C231/12 ,  C07B2200/07 ,  C07C231/16 ,  C07C2601/02 ,  C07C237/04

公开(公告)号：EP1947083A4

公开(公告)日：2009-05-27

申请号：EP06796649

申请日：2006-08-22

申请人： KANEKA CORP

发明人： TAKEDA TOSHIHIRO ,  OHNUKI MASATOSHI ,  KISHIMOTO NARUMI

IPC分类号： C07D207/12

CPC分类号： C07D207/12 ,  Y02P20/55

摘要： Disclosed is a process for production of an aralkyloxypyrrolidine derivative which is important for the production of a pharmaceutical or the like. A 3-aralkyloxypyrrolidine derivative can be produced in the form of a crystal by a process comprising reacting an N-protected-3-hydroxypyrrolidine with a halogenated aralkyl in the presence of a base and a metal halide and/or a phase transfer catalyst to give an N-protected-3-aralkyloxypyrrolidine, performing the deprotection of the N-protecting group in the product to give a 3-aralkyloxypyrrolidine derivative, and treating the product in a solvent containing a polar solvent. The process can produce a highly pure 3-aralkyloxypyrrolidine derivative in a simple manner, with good efficiency, and in an industrial scale.

摘要翻译： 公开了一种生产药物等重要的芳烷氧基吡咯烷衍生物的方法。 3-芳烷氧基吡咯烷衍生物可以通过包括在碱和金属卤化物和/或相转移催化剂存在下使N-保护的-3-羟基吡咯烷与卤代芳烷基反应得到晶体形式，得到 N-保护的-3-芳烷氧基吡咯烷，对产物中的N-保护基进行脱保护得到3-芳烷氧基吡咯烷衍生物，并在含有极性溶剂的溶剂中处理产物。 该方法可以以简单的方式高效纯化并以工业规模生产高纯度的3-芳烷氧基吡咯烷衍生物。

公开(公告)号：EP1300391A4

公开(公告)日：2006-01-04

申请号：EP01941242

申请日：2001-06-26

申请人： KANEKA CORP

发明人： MURAO HIROSHI ,  YAMASHITA KOKI ,  TAKEDA TOSHIHIRO ,  UEDA YASUYOSHI

IPC分类号： C07D263/24 ,  C07B57/00 ,  C07B61/00 ,  C07C227/20 ,  C07C227/32 ,  C07C227/42 ,  C07C229/22 ,  C07C229/34 ,  C07D263/20 ,  C07C227/30 ,  C07B53/00

CPC分类号： C07D263/20 ,  C07C227/20 ,  C07C227/32 ,  C07C227/42 ,  Y02P20/55 ,  C07C229/22 ,  C07C229/34

摘要： An economically advantageous and industrially appropriate process for producing 3-amino-2-hydroxypropionic acid derivatives (1) without resort to any dangerous reagents characterized by comprising treating an N-protected-3-amino-2-hdyroxypropionic acid derivative (2) having a contrary configuration at the carbon atom at the 2-position to a compound (1) with an agent for introducing a leaving group to thereby convert the compound (2) into an N-protected-3-amino-propionic acid derivative (3), then treating the compound (3) with a basic substance to give a substituted 3-amino-2-hydroxypropionic acid derivative (4) having an inversed configuration at the carbon atom at the 2-psoition, and then converting the compound (4) into the 3-amino-2-hydroxypropionic acid derivative (1).

公开(公告)号：EP3124470A4

公开(公告)日：2017-11-01

申请号：EP15769421

申请日：2015-03-23

申请人： KANEKA CORP

发明人： MACHIDA KOJI ,  MORI KOHEI ,  KISHIMOTO NARUMI ,  TAKEDA TOSHIHIRO

IPC分类号： C07C277/08 ,  C07C279/24

CPC分类号： C07C277/08 ,  C07C279/24

摘要： A tri-carbobenzoxy-arginine represented by the following formula (2): is produced by carbobenzoxylating the arginine or arginine derivative (1) represented by the following formula (1), or a salt thereof: by adding carbobenzoxy chloride and a base in a water/organic solvent bilayer system to an arginine or arginine derivative (1) represented by the formula (1), or a salt thereof.

公开(公告)号：EP1457570A4

公开(公告)日：2006-02-01

申请号：EP02788671

申请日：2002-11-28

申请人： KANEKA CORP

发明人： HONDA TATSUYA ,  FUJII AKIO ,  INOUE KENJI ,  YASOHARA YOSHIHIKO ,  ITAGAKI YOSHIFUMI ,  MAEHARA KATSUJI ,  TAKEDA TOSHIHIRO ,  UEDA YASUYOSHI

IPC分类号： C07C213/02 ,  C07C217/74 ,  C07C303/28 ,  C07C309/66 ,  C07C309/73 ,  C12P7/42 ,  C12P41/00 ,  C07B55/00

CPC分类号： C12P7/42 ,  C07B2200/07 ,  C07C213/02 ,  C07C303/28 ,  C07C309/66 ,  C07C309/73 ,  C07C217/74

摘要： The invention relates to simple and efficient preparation of optically active 7-substituted-2-aminotetralins with industrial advantage. A process for preparation of optically active 7- substituted-2-aminotetralins or salts thereof, which comprises reducing a 7-substituted-2-tetralone or a bisulfite adduct thereof with a microorganism into an optically active 7-substituted-2-tetralol, introducing a sulfonyl group into the hydroxyl group of the tetralol to obtain an optically active 7-substituted-2-sulfonyloxytetralin, introducing a nitrogen substituent into the resulting tetralin by the use of a nitrogen nucleophile through inversion to obtain an optically active 2,7-substituted tetralin, and, if necessary, converting the nitrogen substituent into an unsubstituted amino group.

公开(公告)号：EP1481960A4

公开(公告)日：2005-04-06

申请号：EP03737476

申请日：2003-02-04

申请人： KANEKA CORP

发明人： YAMASHITA KOKI ,  TAKEDA TOSHIHIRO ,  UEDA YASUYOSHI

IPC分类号： C07C51/363 ,  C07C51/41 ,  C07C51/43 ,  C07C51/48 ,  C07C51/487 ,  C07C53/19

CPC分类号： C07C51/412 ,  C07C51/363 ,  C07C51/43 ,  C07C53/19

摘要： The invention provides processes for producing efficiently optically active 2-halogenocarboxylic acids useful in the preparation of drugs or the like and salts thereof with amines. Specifically, an optically active 2-halogenocarboxylic acid is produced by halogenating an optically active amino acid in water in the presence of a hydrophobic organic solvent and nitrous acid with the configuration retained and with the racemization inhibited through the removal of 2-hydroxy- bromocarboxylic acid formed as a by-product; the obtained optically active 2-halogenocarboxylic acid is transferred to an aqueous phase by converting it into a salt thereof with a base, followed by the removal of the organic phase; and the optically active 2-halogenocarboxylic acid is transferred again to an organic solvent phase, followed by the removal of the aqueous phase, whereby an optically active 2-halogenocarboxylic acid is obtained through the removal of a halogen component. Further, a high-quality salt of an optically active 2-halogenocarboxylic acid with an amine can be obtained by a crystallization method wherein the amine is added over the period of 1/2 hour or longer either continuously or in portions and/or wherein the crystallization solvent consists of a hydrophobic organic solvent and a hydrophilic organic solvent.

公开(公告)号：EP1403257A4

公开(公告)日：2004-10-13

申请号：EP02728125

申请日：2002-05-23

申请人： KANEKA CORP

发明人： MURAO HIROSHI ,  YAMASHITA KOKI ,  TAKEDA TOSHIHIRO ,  UEDA YASUYOSHI

IPC分类号： C07D263/22 ,  C07D263/24 ,  C07D263/20

CPC分类号： C07D263/24 ,  C07D263/22

摘要： A process for producing, from an N-alkoxycarbonylethylamine compound having an eliminable group in the ß-position, an oxazolidinone derivative of a ß-hydroxyethylamine compound in which the configuration at the ß-position carbon has been inverted, characterized by including the step of contacting with water under acidic to neutral conditions with heating; and a process for producing, from an N-alkoxycarbonylethylamine compound having an eliminable group in the ß-position, a ß-hydroxyethylamine compound in which the configuration at the ß-position carbon has been inverted, characterized in that the oxazolidinone derivative produced above is contacted with water under basic conditions.

摘要翻译： 从β-位具有可消除基团的N-烷氧基羰基乙胺化合物制备其中β位碳上的构型已经被反转的β-羟乙胺化合物的恶唑烷酮衍生物的方法，其特征在于包括以下步骤： 在酸性至中性条件下与水接触并加热; 以及从β位上具有可消除基团的N-烷氧基羰基乙胺化合物制备β-位碳上的​​构型被反转的β-羟乙胺化合物的方法，其特征在于上面制备的恶唑烷酮衍生物是 在碱性条件下与水接触。