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1. 发明申请

US20050170473A1 Process for producing either optically active n-substituted beta-amino acid and optically active n-substituted beta-amino acid ester or optically active n-substituted 2-homopipecolic acid and optically active n-substituted 2-homopipecolic acid ester 失效
标题翻译：用于制备光学活性的n-取代的β-氨基酸和光学活性的n-取代的β-氨基酸酯或光学活性的n-取代的2-同型二烯酸和光学活性的n-取代的2-同型二烯酸酯的方法
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。

2. 发明申请

US20060178433A1 3-Amino-3-arylpropionic acid n-alkyl esters, process for production thereof, and process for production of optically active 3-amino-3-arylpropionic acids and esters of the antipodes thereto 审中-公开
标题翻译： 3-氨基-3-芳基丙酸正烷基酯，其制备方法及其制备光学活性3-氨基-3-芳基丙酸和对映体的酯的方法
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。

3. 发明授权

US07449325B2 Process for enzymatically producing either optically active N-substituted β-amino acids or esters thereof or optically active N-substituted 2-homopipecolic acids or esters thereof 失效
标题翻译：用于酶学产生光学活性N-取代的β-氨基酸或其酯或光学活性N-取代的2-同型二
烯酸或其酯的方法
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。

4. 发明申请

US20050119341A1 3-substituted oxyglutaric diester compound, optically active 3-substituted oxyglutaric monoester compound, and processes for producing these 审中-公开
标题翻译： 3-取代的环戊二酸二酯化合物，光学活性3-取代的氧代戊二酸单酯化合物及其制备方法
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。

5. 发明申请

US20080038785A1 Processes For Preparing Optically Active (S Or R-)-Beta-Amino Acid And Optically Active (R Or S)-Beta-Amino Acid Ester, And Beta-Amino Acid 2-Alkoxyethyl Ester And Optically Active (S Or R)-Beta Amino Acid 2-Alkoxyethyl Ester 有权
标题翻译：制备光学活性（S或R - ） - β-氨基酸和光学活性（R或S） - 氨基酸酯和β-氨基酸2-烷氧基乙酯和光学活性（S或R） - 氨基酸2-烷氧基乙酯
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。

6. 发明授权

US08143052B2 Process for preparing optically active (S or R)-α amino acid and (R or S)-α amino acid ester in one phase organic reaction medium 有权
标题翻译：在一相有机反应介质中制备光学活性（S或R）-α氨基酸和（R或S）-α氨基酸酯）的方法
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。

7. 发明授权

US07915019B2 Processes for preparing optically active (S or R)-β-amino acid and optically active (R or S)-β-amino acid ester, and β-amino acid 2-alkoxyethyl ester and optically active (S or R)-β amino acid 2-alkoxyethyl ester 有权
标题翻译：用于制备光学活性（S或R） - 氨基酸和光学活性（R或S） - 氨基酸酯和和 - 氨基酸2-烷氧基乙酯和光学活性（S或R） - ＆bgr 氨基酸2-烷氧基乙酯
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。

8. 发明申请

US20090117626A1 Process for preparing carboxylic acid using surfactant-modified enzyme 审中-公开
标题翻译：使用表面活性剂改性酶制备羧酸的方法
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。

9. 发明申请

US20090042260A1 PROCESS FOR PREPARING OPTICALLY ACTIVE (S OR R)-ALPHA-AMINO ACID AND OPTICALLY ACTIVE (R OR S)-ALPHA-AMINO ACID ESTER 有权
标题翻译：制备光学活性（S或R） - 氨基酸和光学活性（R或S） - 氨基 - 氨基酸酯的方法
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。

10. 发明授权

US06916792B2 Process for preparing erythromycin compound 失效
标题翻译：红霉素化合物的制备方法
公开(公告)号：US06916792B2
公开(公告)日：2005-07-12
申请号：US10480272
申请日：2002-06-12
申请人： Hiroyuki Miyata , Akira Takama , Tatsuya Kawaguchi , Kazuma Sakata , Kikuo Ataka , Masayoshi Oku , Hiroyuki Suenaga
发明人： Hiroyuki Miyata , Akira Takama , Tatsuya Kawaguchi , Kazuma Sakata , Kikuo Ataka , Masayoshi Oku , Hiroyuki Suenaga
IPC分类号： C07H17/08 , A61K31/7048 , A61K31/70
CPC分类号： C07H17/08
摘要： The present invention is to provide a process for producing a 2′-O-acetyl-4″-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound 4, and it provide a process for producing an erythromycin compound which comprises reacting a formylating agent with a 2′-O-acetylerythromycin A compound 2 to obtain 2-′-O-acetyl-4″-O-formylerythromycin A compound 3, then, acting an acid on Compound 3 to subject to hemiketalation, and then adding an aqueous basic solution in an aqueous solution to precipitate Compound 4 as free crystals.
摘要翻译：本发明提供一种制备2'-O-乙酰基-4'-甲酰基-8,9-脱水红霉素A 6,9-半缩酮化合物4的方法，其提供了一种生产红霉素化合物的方法，其包括使甲酰化试剂与2'-O-乙酰红霉素A化合物2反应，得到2'-乙酰基-4'-O-甲酰基红霉素A化合物3，然后在酸化合物3上进行半缩合反应，然后在水溶液中加入碱性水溶液以将化合物4沉淀为游离结晶。

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