发明申请
US20150166481A1 METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF
审中-公开
用于生产光学活性的3-氨基哌啶或其盐的方法
- 专利标题: METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF
- 专利标题(中): 用于生产光学活性的3-氨基哌啶或其盐的方法
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申请号: US14633622申请日: 2015-02-27
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公开(公告)号: US20150166481A1公开(公告)日: 2015-06-18
- 发明人: Kohei MORI , Masutoshi NOJIRI , Akira NISHIYAMA , Naoaki TAOKA
- 申请人: Kohei MORI , Masutoshi NOJIRI , Akira NISHIYAMA , Naoaki TAOKA
- 申请人地址: JP Osaka
- 专利权人: KANEKA CORPORATION
- 当前专利权人: KANEKA CORPORATION
- 当前专利权人地址: JP Osaka
- 主分类号: C07D211/60
- IPC分类号: C07D211/60 ; C07D211/56
摘要:
The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.