发明申请
US20100087658A1 METHODS AND INTERMEDIATES FOR SYNTHESIS OF SELECTIVE DPP-IV INHIBITORS
审中-公开
合成DPP-IV抑制剂的方法和中间体
- 专利标题: METHODS AND INTERMEDIATES FOR SYNTHESIS OF SELECTIVE DPP-IV INHIBITORS
- 专利标题(中): 合成DPP-IV抑制剂的方法和中间体
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申请号: US12529016申请日: 2008-03-05
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公开(公告)号: US20100087658A1公开(公告)日: 2010-04-08
- 发明人: David Alan Campbell , Emília P.T. Leitão , Zhen-Ping Wu , Peng Wang
- 申请人: David Alan Campbell , Emília P.T. Leitão , Zhen-Ping Wu , Peng Wang
- 申请人地址: US CA San Diego
- 专利权人: Phenomix Corporation
- 当前专利权人: Phenomix Corporation
- 当前专利权人地址: US CA San Diego
- 国际申请: PCT/US08/55927 WO 20080305
- 主分类号: C07F5/02
- IPC分类号: C07F5/02 ; C07D403/12 ; C07D207/00
摘要:
Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.