发明申请
WO2005058794A1 AN IMPROVED PROCESS FOR THE PREPARATION OF TERBINAFINE INTERMEDIATE
审中-公开
一种改进的中草药中间体制剂的改进方法
- 专利标题： AN IMPROVED PROCESS FOR THE PREPARATION OF TERBINAFINE INTERMEDIATE
- 专利标题（中）： 一种改进的中草药中间体制剂的改进方法
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申请号： PCT/IN2003/000394申请日： 2003-12-17
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公开(公告)号： WO2005058794A1公开(公告)日： 2005-06-30
- 发明人: PULLA REDDY, Muddasani , VENKIAH CHOWDARY, Nannapaneni , RAJASEKHARA REDDY, Peddi
- 申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , VENKIAH CHOWDARY, Nannapaneni , RAJASEKHARA REDDY, Peddi
- 申请人地址： Regd office: 'NATCO HOUSE", Road No.2, Banjara Hills, 500 033 Hyderabad, Andhra Pradesh IN
- 专利权人： NATCO PHARMA LIMITED,PULLA REDDY, Muddasani,VENKIAH CHOWDARY, Nannapaneni,RAJASEKHARA REDDY, Peddi
- 当前专利权人： NATCO PHARMA LIMITED,PULLA REDDY, Muddasani,VENKIAH CHOWDARY, Nannapaneni,RAJASEKHARA REDDY, Peddi
- 当前专利权人地址： Regd office: 'NATCO HOUSE", Road No.2, Banjara Hills, 500 033 Hyderabad, Andhra Pradesh IN
- 主分类号： C07C213/08
- IPC分类号： C07C213/08
摘要：
This application discloses an improved process for the preparation of N-methyl-N-(1-naphthylmethyl)-6,6-dimethyl-2-hydroxyheptan-4-ynyl-1-amine, a key intermediate used in the synthesis of terbinafine ((E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethanamine). Process is involving converting tertiary-butylacetylene to its Grignard derivative via transmetallation using lower alkylmagnesium halides and treating it with 1-[N-methyl-N-(1-naphtylmethyl)amino]-2,3-epoxypropane at -10°C to -20°C, slowly heating the reaction mass to reflux temperature and quenching of reaction mass with ammonium chloride to give the compound of the formula-I as crystalline solid.
