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12. 发明申请

US20140127762A1 METHOD FOR PRODUCING OPTICALLY ACTIVE ALPHA-SUBSTITUTED PROLINE 审中-公开
标题翻译：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
申请人： API CORPORATION
发明人： Hisatoshi Uehara , Ryoma Miyake , Keisuke Bando , Hiroshi Kawabata , Tomoko Maeda
IPC分类号： C07D207/16 , C07D207/20
CPC分类号： C07D207/16 , C07D207/20 , C12P13/24 , C12P41/007
摘要： 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.
摘要翻译：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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