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1.发明授权公开(公告)号：US5298660A
公开(公告)日：1994-03-29
申请号：US863976
申请日：1992-04-06
Applicant: Yukio Yoneyoshi , Junko Kudo , Toshio Nishioka
Inventor： Yukio Yoneyoshi , Junko Kudo , Toshio Nishioka
IPC: C07B53/00 , C07B57/00 , C07C213/02 , C07C215/50 , C07C217/58 , C07C251/24 , C07C209/88 , C07C209/40
CPC classification number: C07C217/58 , C07B57/00 , C07C215/50 , C07C251/24 , C07C2101/14
Abstract: Disclosed are optically active secondary amine compounds and salts thereof having the general formula (I): ##STR1## a process for the preparation of the optically active secondary amine compounds and salts thereof, and the use of such compounds. Such compounds exhibit a high resolution power and hence are useful agents for optical resolution.
Abstract translation: 公开了具有通式（I）的光学活性仲胺化合物及其盐：（*化学结构*）（I）制备光学活性仲胺化合物及其盐的方法及其用途。 这样的化合物表现出高分辨率的功率，因此是用于光学分辨率的有用试剂。
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2.发明授权
公开(公告)号：US5510519A
公开(公告)日：1996-04-23
申请号：US165716
申请日：1993-12-13
Applicant: Yukio Yoneyoshi , Junko Kudo , Toshio Nishioka
Inventor： Yukio Yoneyoshi , Junko Kudo , Toshio Nishioka
IPC: C07B53/00 , C07B57/00 , C07C213/02 , C07C215/50 , C07C217/58 , C07C251/24 , C07C209/40 , C07C209/88
CPC classification number: C07C217/58 , C07B57/00 , C07C215/50 , C07C251/24 , C07C2101/14
Abstract: Disclosed are optically active secondary amine compounds and salts thereof having the general formula (I): ##STR1## a process for the preparation of the optically active secondary amine compounds and salts thereof, and the use of such compounds. Such compounds exhibit a high resolution power and hence are useful agents for optical resolution.
Abstract translation: 公开了具有通式（I）的光学活性仲胺化合物及其盐：（I）制备光学活性仲胺化合物及其盐的方法，以及这些化合物的用途。 这样的化合物表现出高分辨率的功率，因此是用于光学分辨率的有用试剂。
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3.发明授权Optically active 4-(tert-butoxycarbonyl)piperazine compound, and method for producing the same 失效光学活性4-（叔丁氧基羰基）哌嗪化合物及其制备方法
公开(公告)号：US06803465B2
公开(公告)日：2004-10-12
申请号：US10076448
申请日：2002-02-19
Applicant: Junko Kudo , Norihiko Hirata , Tomoyasu Yoshida
Inventor： Junko Kudo , Norihiko Hirata , Tomoyasu Yoshida
IPC: C07D295185
CPC classification number: C07D295/073 , C07D295/205
Abstract: A method for producing 1-[(substituted phenyl)phenylmethyl]piperazines useful as intermediates for pharmaceuticals and the like, more particularly, for example, to an intermediate for the production of antiallergic pharmaceuticals. A 4-(tert-butoxycarbonyl)piperazine compound of formula (1): wherein X denotes a chlorine atom, a C1-C3 alkyl group or a C1-C3 alkoxy group, and an optical isomer present therein.
Abstract translation: 可用作药物等的中间体的1 - [（取代苯基）苯甲基]哌嗪的制造方法，特别是例如制备抗过敏药物的中间体。 式（1）的4-（叔丁氧基羰基）哌嗪化合物：其中X表示氯原子，C1-C3烷基或C1-C3烷氧基，以及存在于其中的旋光异构体。
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4.发明授权Process for producing optically active azetidine-2-carboxylic acid derivative 有权光学活性氮杂环丁烷-2-羧酸衍生物的制备方法
公开(公告)号：US06410279B1
公开(公告)日：2002-06-25
申请号：US09619386
申请日：2000-07-19
Applicant: Junko Kudo , Motoo Hazama , Norihiko Hirata
Inventor： Junko Kudo , Motoo Hazama , Norihiko Hirata
IPC: C12P1710
CPC classification number: C12P17/10 , C12P41/005
Abstract: There is provided a process for producing N-substituted azetidine-2-carboxylic acid of the formula I: wherein R1 denotes an aralkyl group or an arylated lower alkoxycarbonyl group and * designates an asymmetric carbon atom, which is characterized by: reacting an N-substituted azetidine-2-carboxylic acid ester of the formula II: wherein R1 has the same meaning as defined above and R2 denotes an alkyl group, an aralkyl group or an allyl group, with an enzyme capable of selectively hydrolyzing a stereoisomer based on the carbon atom of the 2-position of the azetidine ring.
Abstract translation: 提供了制备式I的N-取代的氮杂环丁烷-2-羧酸的方法：其中R1表示芳烷基或芳基化低级烷氧基羰基，*表示不对称碳原子，其特征在于：使N- 取代的氮杂环丁烷-2-羧酸酯，其中R 1具有与上述相同的含义，R 2表示烷基，芳烷基或烯丙基，具有能够基于碳选择性水解立体异构体的酶 氮杂环丁烷2位的原子。
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5.发明授权Method of resolving 2-oxobicyclo [3.1.0] hexane-6-carboxylic acid derivatives 失效拆分2-氧代双环[3.1.0]己烷-6-羧酸衍生物的方法
公开(公告)号：US06407284B1
公开(公告)日：2002-06-18
申请号：US09549564
申请日：2000-04-14
Applicant: Junko Kudo , Yoshiki Takashima , Sanae Mine
Inventor： Junko Kudo , Yoshiki Takashima , Sanae Mine
IPC: C07B5500
CPC classification number: C12P7/40 , C12N9/18 , C12P41/005
Abstract: There is disclosed a method of resolving 2-oxobicyclo[3.1.0]hexane-6-carboxylates having the following relative configuration of formula (1): wherein X1, X2, R1, R2 and R3 have the same meanings as defined below, into one enantiomer ester thereof and the other enantiomer acid, which is characterized by contacting an enzyme having an ability to preferentially hydrolyze one enantiomer ester contained in 2-oxobicyclo[3.1.0]hexane-6-carboxylate of formula (1) as defined above, with 2-oxobicyclo[3.1.0]hexane-6-carboxylates of formula (1) as defined above to obtain one enantiomer as an acid and the other enantiomer as an ester.
Abstract translation: 公开了具有以下式（1）的相对构型的2-氧代双环[3.1.0]己烷-6-羧酸盐的方法：其中X1，X2，R1，R2和R3具有如下定义的相同含义， 一种对映异构体酯和另一种对映异构体酸，其特征在于将具有如上定义的式（1）的2-氧代双环[3.1.0]己烷-6-羧酸酯中所含的一种对映体酯的能力优先水解的酶与下式的酶接触： 如上定义的式（1）的2-氧代双环[3.1.0]己烷-6-羧酸酯，得到一种对映异构体，为酸，另一种对映体为酯。
![Method of resolving 2-oxobicyclo [3.1.0] hexane-6-carboxylic acid derivatives](/docs/US/2002-06-18/US06407284B1/abs.jpg.600x600.jpg)
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6.发明授权Process for producing optically active azetidine-2-carboxylic acid derivative 失效光学活性氮杂环丁烷-2-羧酸衍生物的制备方法
公开(公告)号：US06162621A
公开(公告)日：2000-12-19
申请号：US12227
申请日：1998-01-23
Applicant: Junko Kudo , Motoo Hazama , Norihiko Hirata
Inventor： Junko Kudo , Motoo Hazama , Norihiko Hirata
CPC classification number: C12P17/10 , C12P41/005
Abstract: There is provided a process for producing N-substituted azetidine-.2-carboxylic acid of the formula I: ##STR1## wherein R.sup.1 denotes an aralkyl group or an arylated lower alkoxycarbonyl group and * designates an asymmetric carbon atom, which is characterized by:reacting an N-substituted azetidine-2-carboxylic acid ester of the formula II: ##STR2## wherein R.sup.1 has the same meaning as defined above and R.sup.2 denotes an alkyl group, an aralkyl group or an allyl group, with an enzyme capable of selectively hydrolyzing a stereoisomer based on the carbon atom of the 2-position of the azetidine ring.
Abstract translation: 提供了制备式I的N-取代的氮杂环丁烷-2-羧酸的方法：其中R1表示芳烷基或芳基化低级烷氧基羰基，*表示不对称碳原子，其特征在于：使N 取代的氮杂环丁烷-2-羧酸酯：其中R 1具有与上述相同的含义，并且R 2表示烷基，芳烷基或烯丙基，具有能够选择性地水解立体异构体的酶基于 氮原子环的2位的碳原子。
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7.发明授权Process for producing optically active n-substituted azetidine-2 carboxylic acid compound 失效光学活性的n-取代的氮杂环丁烷-2-羧酸化合物的制备方法
公开(公告)号：US6143554A
公开(公告)日：2000-11-07
申请号：US352350
申请日：1999-07-13
Applicant: Yoshiki Takashima , Junko Kudo , Ayumi Inoue , Motoo Hazama
Inventor： Yoshiki Takashima , Junko Kudo , Ayumi Inoue , Motoo Hazama
CPC classification number: C07D205/04 , C12P41/005
Abstract: There is provided a process for producing an optically active N-substituted azetidine-2-carboxylic acid compound represented by the formula (2): ##STR1## by contacting a corresponding N-substituted azetidine-2-carboxylic acid ester of formula (2) with an enzyme derived from a microorganism selected from Arthrobacter SC-6-98-28 strain, Arthrobacter sp. ATCC21908 strain, Chromobacterium SC-YM-1 strain, and a mutant thereof. A process is also provided for preparing an optically active azetidine-2-carboxylic acid by eliminating the N-substituent of a N-substituted azetidine-2-carboxylic acid ester of formula (2).
Abstract translation: 提供了制备由式（2）表示的光学活性的N-取代的氮杂环丁烷-2-羧酸化合物的方法：将式（2）的相应的N-取代的氮杂环丁烷-2-羧酸酯与酶 衍生自选自节杆菌SC-6-98-28菌株，节杆菌属（Arthrobacter sp。）的微生物 ATCC21908菌株，Chromobacterium SC-YM-1菌株及其突变体。 还提供了通过除去式（2）的N-取代的氮杂环丁烷-2-羧酸酯的N-取代基来制备光学活性氮杂环丁烷-2-羧酸的方法。
