发明授权
EP1756049B1 VERFAHREN ZUR HERSTELLUNG VON 1,4-DIPHENYLAZETIDINON-DERIVATEN
有权
用于生产1,4- diphenylazetidinone衍生物
- 专利标题: VERFAHREN ZUR HERSTELLUNG VON 1,4-DIPHENYLAZETIDINON-DERIVATEN
- 专利标题(英): Method for producing 1,4-diphenyl azetidinone derivatives
- 专利标题(中): 用于生产1,4- diphenylazetidinone衍生物
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申请号: EP05747892.7申请日: 2005-05-20
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公开(公告)号: EP1756049B1公开(公告)日: 2007-10-31
- 发明人: LINDENSCHMIDT, Andreas , WILL, David, William , JAEHNE, Gerhard , WOLLMANN, Theodor, Andreas , FRICK, Wendelin , JUNKER, Bernd , RIGAL, David , BILLEN, Guenter , JENDRALLA, Heiner
- 申请人: Sanofi-Aventis Deutschland GmbH
- 申请人地址: Brüningstrasse 50 65929 Frankfurt am Main DE
- 专利权人: Sanofi-Aventis Deutschland GmbH
- 当前专利权人: Sanofi-Aventis Deutschland GmbH
- 当前专利权人地址: Brüningstrasse 50 65929 Frankfurt am Main DE
- 优先权: DE102004025071 20040521; DE102005010770 20050309
- 国际公布: WO2005113496 20051201
- 主分类号: C07D205/08
- IPC分类号: C07D205/08
摘要:
The invention relates to a method for producing 1,4-diphenyl azetidinone derivatives from suitably protected β-substituted amino amides, in the presence of silylation agents. Said method uses cyclization catalysts that comprise phosphonium ions as the cation of formula (XII), and ions of the following general formulas (a), (b), (c) or (d) as the anion. In said formulas, the symbols, substituents and indices are defined as follows: Z = C=O, C=S, S=O, SO2 or C=NR20; K = O, S, NR21 or CR22R23; L = NR24 or CR25R26; n = 0 or 1; M = O, C=O, NR27 or CR28R29; Q = O, S, NR30, CR31R32, C=O, C=S, S=O, SO2 or C=NR34; R = CR35 or N; T = CR36 or N; U = CR37 or N; V = CR38 or N; the groups R16 to R19 can represent, for example, aryl or (C1-C15) alkyl, aryl(C1-C10)alkene, and the groups R20 to R32 and R34 to R38 can represent in addition H or heteroaryl; R39 and R40 represent, for example (C1-C6) alkyl. The anion can also be R41O-, R42COO- or Cl-, Br- or I- (combined with Ag2O).
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