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    METHOD FOR PRODUCING a-SUBSTITUTED CYSTEINE OR SALT THEREOF OR SYNTHETIC INTERMEDIATE OF a-SUBSTITUTED CYSTEINE
    3.
    发明申请
    METHOD FOR PRODUCING a-SUBSTITUTED CYSTEINE OR SALT THEREOF OR SYNTHETIC INTERMEDIATE OF a-SUBSTITUTED CYSTEINE 审中-公开
    生产取代的CYSTEINE或其盐的方法或其取代的CYSTEINE的合成中间体

    公开(公告)号：US20160083341A1

    公开(公告)日：2016-03-24

    申请号：US14888576

    申请日：2014-05-01

    Applicant: API Corporation

    Inventor： Yuuki Asuma ,  Hisatoshi Uehara ,  Tomoko Maeda ,  Yasuyo Saito ,  Ryoma Miyake ,  Hiroshi Kawabata

    IPC: C07C319/06 ,  C07C323/52 ,  C12P13/12 ,  C07C323/58 ,  C07D277/14 ,  C07C319/14 ,  C07C319/20 ,  C07C323/60

    CPC classification number: C07C319/06 ,  C07C319/02 ,  C07C319/14 ,  C07C319/20 ,  C07C323/52 ,  C07C323/58 ,  C07C323/60 ,  C07D277/14 ,  C12P13/12 ,  C07C323/12 ,  C07C323/03

    Abstract: According to the present invention, it becomes possible to perform a process for converting into an α-substituted cysteine represented by general formula (1) or a salt thereof at low cost and on an industrial scale by employing a process that is routed through a compound represented by general formula (3) to a compound represented by general formula (6). Particularly, by employing a process that is routed through a compound represented by general formula (7-2), it becomes possible to detach a tert-butyl protection group in a simple manner and to produce the compound represented by general formula (1) with high purity. Furthermore, by employing a process that is routed through tert-butylthiomethanol or a process that is routed through a compound represented by general formula (9), it becomes possible to produce a compound represented by general formula (2) without generating bischloromethylether that is an oncogenic substance. In the production of an α-substituted-D-cysteine or a salt thereof, it becomes possible to perform a process for converting the compound represented by general formula (2) into a compound represented by general formula (3S) in one step by allowing an enzyme or the like to act on the compound represented by general formula (2).

    Abstract translation: 根据本发明，可以通过使用通过化合物的方法，以低成本和工业规模进行转化成由通式（1）表示的α-取代的半胱氨酸或其盐的方法 由通式（3）表示的化合物与通式（6）表示的化合物反应。 特别是通过使用通过通式（7-2）表示的化合物的方法，可以简单地分离叔丁基保护基，并制备通式（1）表示的化合物与 高纯度 此外，通过使用通过叔丁基硫醇的方法或通过通式（9）表示的化合物的方法，可以生成由通式（2）表示的化合物，而不产生作为 致癌物质。 在制备α-取代-D-半胱氨酸或其盐时，可以通过以下步骤进行将由通式（2）表示的化合物转化为通式（3S）表示的化合物的方法：允许 酶等作用于由通式（2）表示的化合物。

    Method for Producing cis-5-hydroxy-2-piperidinecarboxylic Acid Derivative, and Method for Purifying cis-5-hydroxy-2-piperidinecarboxylic Acid
    4.
    发明申请
    Method for Producing cis-5-hydroxy-2-piperidinecarboxylic Acid Derivative, and Method for Purifying cis-5-hydroxy-2-piperidinecarboxylic Acid 有权
    顺式-5-羟基-2-哌啶羧酸衍生物的制备方法以及顺式-5-羟基-2-哌啶羧酸的纯化方法

    公开(公告)号：US20150239906A1

    公开(公告)日：2015-08-27

    申请号：US14431141

    申请日：2013-12-19

    Applicant: API CORPORATION

    Inventor： Tomoko Maeda ,  Hisatoshi Uehara ,  Yasuyo Saito ,  Masato Murai

    IPC: C07D498/08 ,  C07D211/60

    CPC classification number: C07D498/08 ,  C07D211/60 ,  C12P17/12 ,  Y02P20/55

    Abstract: The present invention aims to provide a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid with high purity, and a method for producing its derivative. The present invention provides a method for producing a cis-5-hydroxy-2-piperidinecarboxylic acid derivative, which method comprises a step of converting cis-5-hydroxy-2-piperidinecarboxylic acid into a compound(s) of Formula (1) and/or Formula (2) (wherein R1 represents a protective group for an amino group, and R2 represents a C1-C6 alkyl group), and a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid.

    Abstract translation: 本发明旨在提供一种纯度高的顺式-5-羟基-2-哌啶羧酸的纯化方法及其衍生物的制造方法。 本发明提供了顺式-5-羟基-2-哌啶羧酸衍生物的制备方法，该方法包括将顺式-5-羟基-2-哌啶羧酸转化成式（1）的化合物和 /或式（2）（其中R1表示氨基的保护基，R2表示C1-C6烷基）和顺式-5-羟基-2-哌啶羧酸的纯化方法。

    METHOD FOR PRODUCING OPTICALLY ACTIVE ALPHA-SUBSTITUTED PROLINE
    6.
    发明申请
    METHOD FOR PRODUCING OPTICALLY ACTIVE ALPHA-SUBSTITUTED PROLINE 审中-公开
    用于生产光学活性的ALPHA取代基的方法

    公开(公告)号：US20140127762A1

    公开(公告)日：2014-05-08

    申请号：US14122365

    申请日：2012-03-29

    Applicant: API CORPORATION

    Inventor： Hisatoshi Uehara ,  Ryoma Miyake ,  Keisuke Bando ,  Hiroshi Kawabata ,  Tomoko Maeda

    IPC: C07D207/16 ,  C07D207/20

    CPC classification number: C07D207/16 ,  C07D207/20 ,  C12P13/24 ,  C12P41/007

    Abstract: The present invention aims to provide an industrial method practically suitable for producing optically active α-substituted prolines from an acyclic ketone compound by a small number of steps under mild conditions. The present invention relates to a production method of an optically active α-substituted proline (4) and/or an optically active α-substituted prolinamide (5), including (a) reacting an acyclic ketone compound (1) with at least one selected from ammonia, an ammonium salt, primary amine and a salt of primary amine, and a cyanating agent to give a cyclic nitrogen-containing compound (2), (b) hydrating the cyclic nitrogen-containing compound (2) to give an α-substituted prolinamide (3), and (c) resolving the α-substituted prolinamide (3) by one or more of (d) enzymatical hydrolysis, (e) resolution by diastereomeric salt formation, and (f) separation by column chromatography.

    Abstract translation: 本发明旨在提供一种实际上适用于在温和条件下通过少量步骤从无环酮化合物制备光学活性α-取代的脯氨酸的工业方法。 本发明涉及光学活性α-取代脯氨酸（4）和/或光学活性α-取代脯氨酰胺（5）的制备方法，包括（a）使无环酮化合物（1）与至少一种选择的 由氨，铵盐，伯胺和伯胺的盐和氰化剂得到环状含氮化合物（2），（b）使环状含氮化合物（2）水合，得到α- 取代的脯氨酰胺（3），和（c）通过（d）酶水解，（e）通过非对映异构体盐形成的拆分，和（f）通过柱色谱法分离的α-取代的脯氨酰胺（3）

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