发明授权
- 专利标题： Formation of tetra-substituted enamides and stereoselective reduction thereof
- 专利标题（中）： 四取代烯酰胺的形成及其立体选择性还原
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申请号： US11629005申请日： 2005-07-01
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公开(公告)号： US07629470B2公开(公告)日： 2009-12-08
- 发明人: Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
- 申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
- 申请人地址： US NJ Rahway
- 专利权人： Merck & Co., Inc.
- 当前专利权人： Merck & Co., Inc.
- 当前专利权人地址： US NJ Rahway
- 代理商 Baerbel R. Brown; Catherine D. Fitch
- 国际申请： PCT/US2005/023514 WO 20050701
- 国际公布： WO2006/017045 WO 20060216
- 主分类号： C07D213/63
- IPC分类号： C07D213/63
摘要：
The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
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