发明授权
EP1758879B1 METHOD OF MANUFACTURING (S)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE)
有权
工艺用于制备（S）-N-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺盐酸盐（度洛西汀）
- 专利标题： METHOD OF MANUFACTURING (S)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE)
- 专利标题（中）： 工艺用于制备（S）-N-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺盐酸盐（度洛西汀）
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申请号： EP05793945.6申请日： 2005-10-21
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公开(公告)号： EP1758879B1公开(公告)日： 2007-12-12
- 发明人: RIDVAN, Ludek , HRUBY, Petr , PLACEK, Lukas , KUCHAR, Miroslav
- 申请人： Zentiva, a.s.
- 申请人地址： U kabelovny 130 102 37 Praha 10 CZ
- 专利权人： Zentiva, a.s.
- 当前专利权人： Zentiva, a.s.
- 当前专利权人地址： U kabelovny 130 102 37 Praha 10 CZ
- 代理机构： Jirotkova, Ivana
- 优先权： CZ20041072 20041026
- 国际公布： WO2006045255 20060504
- 主分类号： C07D333/20
- IPC分类号： C07D333/20 ; A61K31/38
摘要：
A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)-N,N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (III) is reacted with an optically active acid, after which a crystallization is made of that diastereoisomer which yields, by reaction with an inorganic or organic base, (S)-N,N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (S)-III, which is then demethylated using alkylchloroformates, followed by a hydrolysis and optional conversion of the compound of formula (I) to its salt.
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