发明授权
- 专利标题: Method for preparing phenyloxymethyl-nitro-imidazole derivatives and use of same
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申请号: US14647017申请日: 2012-11-22
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公开(公告)号: US09758488B2公开(公告)日: 2017-09-12
- 发明人: Zsolt Parkanyi , Edit Alattyani , Zoltan Bugir , Marton Harsanyi
- 申请人: SANOFI
- 申请人地址: FR Paris
- 专利权人: SANOFI
- 当前专利权人: SANOFI
- 当前专利权人地址: FR Paris
- 代理机构: Morrison & Foerster LLP
- 国际申请: PCT/EP2012/073321 WO 20121122
- 国际公布: WO2014/079497 WO 20140530
- 主分类号: C07D233/94
- IPC分类号: C07D233/94
摘要:
Fexinidazole is prepared according to a method which comprises the following steps: a) reacting 1-methyl-2-hydroxymethyl-5-nitro-imidazole with methanesulfonyl chloride in the presence of a suspension of powdered alkaline carbonate in an anhydrous organic solvent suitable for performing nucleophile substitution reactions; b) adding to the resulting reaction medium a solution of 4-methyl-mercapto-phenol in the same organic solvent as referred to in step a); c) separating fexinidazole from the reaction mixture as its hydrochloride salt and d) converting said hydrochloride salt into fexinidazole and optionally, purifying the latter.
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