发明授权
- 专利标题: BENZENESULPHONAMIDES AND PROCESS FOR THEIR PREPARATION
- 专利标题(中): Benzenesulphonamides及其制备方法
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申请号: EP03793925.3申请日: 2003-09-08
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公开(公告)号: EP1539684B1公开(公告)日: 2009-04-15
- 发明人: GIZUR, Tibor , TÖRLEY, Jozsef , FOGASSY, Elemér , BALINT, Jozsef , EGRI, Gabriella , DEMETER, Adám
- 申请人: Richter Gedeon Nyrt.
- 申请人地址: Gyömröi út 19-21 1103 Budapest HU
- 专利权人: Richter Gedeon Nyrt.
- 当前专利权人: Richter Gedeon Nyrt.
- 当前专利权人地址: Gyömröi út 19-21 1103 Budapest HU
- 优先权: HU0202963 20020909
- 国际公布: WO2004022532 20040318
- 主分类号: C07C303/40
- IPC分类号: C07C303/40 ; C07C311/37 ; A61K31/18
摘要:
New process for industrial preparation of R-(-)-tamsulosine HCl of formula (I). In this process (R,S)-5-[2-(N-benzyl-amino)-propyl]-2-methoxy-benzenesulphonamide of formula (I), acid addition salts and enantiomers thereof and R-5-[2-[N-(2-ethoxy-phenoxy)-ethyl]-N-benzyl]-amino]-propyl-2-methoxy-benzenesulphonamide of formula (III) are new intermediates. R-(-)-tamsulosine HCl of formula (I) is prepared by reacting the secondary benzylamine of formula (II) with an alkylating agent to R-5-[2-[N-(2-ethoxy-phenoxy)-ethyl]-N-benzyl]-amino]-propyl-2-methoxy-benzenesulphonamide of formula (III), the benzyl protecting group is removed and then HCl salt is formed. The optically active compound of formula (II) is prepared by reductive condensation of (4-methoxy-3-sulphamoyl-phenyl)-acetone and benzylamine and the obtained racemic compound is optically resolved by chiral acid.
公开/授权文献
- EP1539684A1 BENZENESULPHONAMIDES AND PROCESS FOR THEIR PREPARATION 公开/授权日:2005-06-15
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