发明公开
EP2123769A1 METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF
有权
工艺生产光学活性的3-氨基哌啶或其盐
- 专利标题: METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF
- 专利标题(中): 工艺生产光学活性的3-氨基哌啶或其盐
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申请号: EP08711442.7申请日: 2008-02-18
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公开(公告)号: EP2123769A1公开(公告)日: 2009-11-25
- 发明人: MORI, Kohei , NOJIRI, Masutoshi , NISHIYAMA, Akira , TAOKA, Naoaki
- 申请人: Kaneka Corporation
- 申请人地址: 2-4, Nakanoshima 3-chome Kita-ku Osaka-shi, Osaka 530-8288 JP
- 专利权人: Kaneka Corporation
- 当前专利权人: Kaneka Corporation
- 当前专利权人地址: 2-4, Nakanoshima 3-chome Kita-ku Osaka-shi, Osaka 530-8288 JP
- 代理机构: Vossius & Partner
- 优先权: JP2007037598 20070219
- 国际公布: WO2008102720 20080828
- 主分类号: C12P41/00
- IPC分类号: C12P41/00 ; C07D211/56 ; C07D211/60 ; C07B57/00
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.
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