公开(公告)号：US20080038785A1

公开(公告)日：2008-02-14

申请号：US11664878

申请日：2005-10-11

申请人： Tadayoshi Konegawa ,  Hiroyuki Miyata ,  Yasuhito Yamamoto

发明人： Tadayoshi Konegawa ,  Hiroyuki Miyata ,  Yasuhito Yamamoto

IPC分类号： C12P13/04

CPC分类号： C12P41/005 ,  C07C227/18 ,  C07C229/34 ,  C12P13/04 ,  C12P13/222

摘要： The present invention relates to a process for preparing an optically active (S or R)-β-amino acid represented by the formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, aryl group or heteroaryl group each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-β-amino acid ester represented by the formula (III): wherein R has the same meaning as defined above, R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has a reverse absolute configuration to that of the compound of the formula (II), which comprises selectively hydrolyzing water and one of enantiomers of a β-amino acid ester represented by the formula (I): wherein R and R1 have the same meanings as defined above, which is a racemic mixture, in the presence of a hydrolase in an organic solvent.

摘要翻译： 本发明涉及一种制备由式（II）表示的光学活性（S或R） - 氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，芳基 基团或杂芳基，其各自可以具有取代基，*表示不对称碳原子，以及由式（III）表示的光学活性（R或S） - 氨基酸酯：其中R具有 与上述相同的含义，R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有相对于化合物的反向绝对构型 式（II）包括选择性地水解由式（I）表示的β-氨基酸酯的水和一种对映体：其中R和R 1具有与上述相同的含义， 其是在有机溶剂中的水解酶存在下的外消旋混合物。

公开(公告)号：US20050170473A1

公开(公告)日：2005-08-04

申请号：US10510483

申请日：2003-04-08

申请人： Hiroyuki Miyata ,  Yasuhito Yamamoto ,  Tadayoshi Konegawa ,  Kazuma Sakata

发明人： Hiroyuki Miyata ,  Yasuhito Yamamoto ,  Tadayoshi Konegawa ,  Kazuma Sakata

IPC分类号： C12P13/04 ,  C12P41/00 ,  C07C229/02

CPC分类号： C12P41/005 ,  C12P13/04

摘要： The present invention discloses a process which comprises selectively hydrolyzing one enantiomer of racemic mixtures of an N-substituted β-amino acid alkyl ester or N-substituted 2-homopipecolic acid ester represented by the formula (I): wherein Ar, R1, R2, R3, R4 and R5 are the same as defined in the specification, in the presence of a hydrolase to form an optically active ((R) or (S))-N-substituted-β-amino acid or optically active ((R) or (S))-N-substituted 2-homopipecolic acid represented by the formula (II): and simultaneously to obtain an unreacted optically active ((S) or (R))-N-substituted β-amino acid alkyl ester or unreacted optically active ((S) or (R))-N-substituted 2-homopipecolic acid ester represented by the formula (III): which has a reverse steric absolute configuration to that of the compound represented by the formula (II).

摘要翻译： 本发明公开了一种方法，其包括选择性水解由式（I）表示的N-取代的β-氨基酸烷基酯或N-取代的2-同型二酸酸酯的外消旋混合物的一种对映异构体：其中Ar， 1，R 2，R 3，R 4和R 5与定义的相同 在说明书中，在水解酶存在下形成光学活性（（R）或（S））-N-取代的β-氨基酸或光学活性（（R）或（S））-N-取代的2 同时获得未反应的光学活性（（S）或（R））-N-取代的β-氨基酸烷基酯或未反应的光学活性的（（S）或（R）） - ）由式（III）表示的-N-取代的2-同型二烯酸酯：其具有与式（II）表示的化合物的反空间绝对构型。

公开(公告)号：US07449325B2

公开(公告)日：2008-11-11

申请号：US10510483

申请日：2003-04-08

申请人： Hiroyuki Miyata ,  Yasuhito Yamamoto ,  Tadayoshi Konegawa ,  Kazuma Sakata

发明人： Hiroyuki Miyata ,  Yasuhito Yamamoto ,  Tadayoshi Konegawa ,  Kazuma Sakata

IPC分类号： C12P41/00 ,  C12P13/04

CPC分类号： C12P41/005 ,  C12P13/04

摘要： The present invention discloses a process which comprises selectively hydrolyzing one enantiomer of racemic mixtures of an N-substituted β-amino acid alkyl ester or N-substituted 2-homopipecolic acid ester represented by the formula (I): wherein Ar, R1, R2, R3, R4 and R5 are the same as defined in the specification, in the presence of a hydrolase to form an optically active ((R) or (S))—N-substituted β-amino acid or optically active ((R) or (S))—N-substituted 2-homopipecolic acid represented by the formula (II): and simultaneously to obtain an unreacted optically active ((S) or (R))—N-substituted β-amino acid alkyl ester or unreacted optically active ((S) or (R))—N-substituted 2-homopipecolic acid ester represented by the formula (III): which has a reverse steric absolute configuration to that of the compound represented by the formula (II).

摘要翻译： 本发明公开了一种方法，其包括选择性水解由式（I）表示的N-取代的β-氨基酸烷基酯或N-取代的2-同型二酸酸酯的外消旋混合物的一种对映异构体：其中Ar， 1，R 2，R 3，R 4和R 5与定义的相同 在说明书中，在水解酶的存在下，形成光学活性（（R）或（S））-N-取代的β-氨基酸或光学活性（（R）或（S））-N-取代的2- 同时获得未反应的光学活性（（S）或（R））-N-取代的β-氨基酸烷基酯或未反应的光学活性（（S）或（R）） 由式（III）表示的N-取代的2-同型二烯酸酯：其具有与由式（II）表示的化合物的反方位绝对构型。

公开(公告)号：US20050119341A1

公开(公告)日：2005-06-02

申请号：US10511674

申请日：2003-04-18

申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Kazuma Sakata

发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Kazuma Sakata

IPC分类号： C07C68/02 ,  C07C69/96 ,  A61K31/225

CPC分类号： C07C69/96 ,  C07B2200/07 ,  C07C68/02

摘要： The present invention is to provide a 3-substituted oxyglutaric acid diester compound represented by the following formula (I): wherein R1 may be the same or different from each other, and represents a substituted or unsubstituted alkyl group, R2 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group, and an optically active 3-substituted oxyglutaric acid monoester compound represented by the following formula (IV): wherein R1 and R2 have the same meanings as defined above, and processes for preparing the same.

摘要翻译： 本发明提供由下式（I）表示的3-取代的环戊二酸二酯化合物：其中R 1彼此可以相同或不同，并且表示取代或未取代的烷基 基团R 2表示取代或未取代的烷基，取代或未取代的烯基，取代或未取代的芳烷基或取代或未取代的芳基，和光学活性3-取代的氧戊二酸单酯 由下式（IV）表示的化合物：其中R 1和R 2具有与上述相同的含义及其制备方法。

公开(公告)号：US08143052B2

公开(公告)日：2012-03-27

申请号：US12064589

申请日：2006-08-25

申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

IPC分类号： C12P41/00

CPC分类号： C12P13/04 ,  C12P41/005

摘要： The present invention discloses a process for preparing an optically active (S or R)-α-amino acid represented by the formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, heteroarylalkyl group, aryl group or heteroaryl group, each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-α-amino acid ester represented by the formula (III): wherein R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has an opposite absolute configuration to that of the compound of the formula (II), which comprises selectively reacting water with one of enantiomers of an α-amino acid ester which is a racemic mixture and represented by the formula (I): wherein R and R1 have the same meanings as defined above, in the presence of a lipase or a protease in an organic solvent.

摘要翻译： 本发明公开了一种制备由式（II）表示的光学活性（S或R）-α-氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，杂芳基烷基 ，芳基或杂芳基，每个可以具有取代基，*表示不对称碳原子，和由式（III）表示的光学活性（R或S）-α-氨基酸酯：其中 R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有与式（II）化合物相反的绝对构型，其包括选择性地使水与 由式（I）表示的α-氨基酸酯的对映异构体：其中R和R 1具有与上述相同的含义，在有机溶剂中存在脂肪酶或蛋白酶的情况下。

公开(公告)号：US20060178433A1

公开(公告)日：2006-08-10

申请号：US10549322

申请日：2004-03-17

申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Kazuma Sakata

发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Kazuma Sakata

IPC分类号： A61K31/24 ,  C07C229/34

CPC分类号： C12P41/005 ,  C07B2200/07 ,  C07C229/34 ,  C07D317/60 ,  C12P13/04

摘要： The present invention is to provide an n-alkyl 3-amino-3-arylpropionate represented by the formula (I): wherein Ar1 represents an aryl group which may have a substituent(s), provided that a phenyl group and 4-methoxyphenyl group are excluded, R1 represents an n-propyl group or an n-butyl group, and a process for preparing the same, and its optically active compound and an optically active (S or R)-3-amino-3-arylpropionic acid represented by the formula (III-a): wherein Ar represents an aryl group which may have a substituent(s), and * represents an asymmetric carbon, and a process for preparing an optically active n-alkyl (R or S)-3-amino-3-arylpropionate represented by the formula (IV-a): wherein Ar and R1 have the same meanings as defined above, * represents an asymmetric carbon, provided that it has a reverse absolute configuration to the compound of the formula (III-a).

摘要翻译： 本发明提供由式（I）表示的3-氨基-3-芳基丙酸正烷基酯：其中Ar 1表示可以具有取代基的芳基，条件是 除了苯基和4-甲氧基苯基之外，R 1表示正丙基或正丁基，及其制备方法，其光学活性化合物和光学活性化合物 由式（III-a）表示的（S或R）-3-氨基-3-芳基丙酸：其中Ar表示可以具有取代基的芳基，*表示不对称碳， 制备由式（IV-a）表示的光学活性正烷基（R或S）-3-氨基-3-芳基丙酸酯：其中Ar和R 1具有与上述相同的含义， *表示不对称碳，条件是其具有与式（III-a）化合物相反的绝对构型。

公开(公告)号：US07915019B2

公开(公告)日：2011-03-29

申请号：US11664878

申请日：2005-10-11

申请人： Tadayoshi Konegawa ,  Hiroyuki Miyata ,  Yasuhito Yamamoto

发明人： Tadayoshi Konegawa ,  Hiroyuki Miyata ,  Yasuhito Yamamoto

IPC分类号： C12P13/00 ,  C07B55/00

CPC分类号： C12P41/005 ,  C07C227/18 ,  C07C229/34 ,  C12P13/04 ,  C12P13/222

摘要： A process for preparing an optically active (S or R)-β-amino acid represented by formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, aryl group or heteroaryl group each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-β-amino acid ester represented by formula (III): wherein R has the same meaning as defined above, R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has a reverse absolute configuration to that of the compound of the formula (II), which comprises selectively hydrolyzing water and one of enantiomers of a β-amino acid ester represented by formula (I): wherein R and R1 have the same meanings as defined above, which is a racemic mixture, in the presence of a hydrolase in an organic solvent.

摘要翻译： 一种制备由式（II）表示的光学活性（S或R） - 氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，芳基或杂芳基 其可以具有取代基，*表示不对称碳原子，以及由式（III）表示的光学活性（R或S） - （ - ） - 氨基酸酯：其中R具有与上述相同的含义 R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有与式（II）化合物相反的绝对构型，其包括选择性水解水和一种 由式（I）表示的α-氨基酸酯的对映异构体：其中R和R 1具有与上述定义相同的含义，其是在有机溶剂中的水解酶存在下的外消旋混合物。

公开(公告)号：US20090117626A1

公开(公告)日：2009-05-07

申请号：US11920571

申请日：2006-05-17

申请人： Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Yasuhito Yamamoto

发明人： Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Yasuhito Yamamoto

IPC分类号： C12P13/00

CPC分类号： C12P7/52 ,  C12N9/20 ,  C12P13/001 ,  C12P13/04 ,  C12P41/005

摘要： The present invention relates to a process for preparing a carboxylic acid using a surfactant-modified enzyme which comprises selectively reacting water and a carboxylic acid ester, provided that triglyceride is excluded, in an organic solvent in the presence of a surfactant-modified enzyme.

摘要翻译： 本发明涉及一种使用表面活性剂改性酶制备羧酸的方法，该方法包括在表面活性剂改性酶存在下，在有机溶剂中选择性地使水和羧酸酯反应，条件是甘油三酸酯被排除。

公开(公告)号：US20090042260A1

公开(公告)日：2009-02-12

申请号：US12064589

申请日：2006-08-25

申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

IPC分类号： C12P13/04

CPC分类号： C12P13/04 ,  C12P41/005

摘要： The present invention discloses a process for preparing an optically active (S or R)-α-amino acid represented by the formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, heteroarylalkyl group, aryl group or heteroaryl group, each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-α-amino acid ester represented by the formula (III): wherein R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has an opposite absolute configuration to that of the compound of the formula (II), which comprises selectively reacting water with one of enantiomers of an α-amino acid ester which is a racemic mixture and represented by the formula (I): wherein R and R1 have the same meanings as defined above, in the presence of a lipase or a protease in an organic solvent.

摘要翻译： 本发明公开了一种制备由式（II）表示的光学活性（S或R）-α-氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，杂芳基烷基 ，芳基或杂芳基，每个可以具有取代基，*表示不对称碳原子，和由式（III）表示的光学活性（R或S）-α-氨基酸酯：其中 R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有与式（II）化合物相反的绝对构型，其包括选择性地使水与 由式（I）表示的外消旋混合物的α-氨基酸酯的对映异构体：其中R和R 1具有与上述相同的含义，在有机溶剂中存在脂肪酶或蛋白酶。