发明公开
- 专利标题： PROCEDE DE SYNTHESE DE DERIVES D'ACIDE HYDROXY-BISPHOSPHONIQUE
- 专利标题（英）： Method for synthesizing hydroxy-bisphosphonic acid derivatives
- 专利标题（中）： 用于合成羟基二膦酸衍生物的方法
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申请号： EP09700083.0申请日： 2009-01-05
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公开(公告)号： EP2240500A1公开(公告)日： 2010-10-20
- 发明人: EGOROV, Maxim , FORTUN, Yannick , HEYMANN, Dominique , LEBRETON, Jacques , MATHE, Monique , PADRINES, Marc , REDINI, Françoise
- 申请人： Université de Nantes , Chu Nantes , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , Centre National de la Recherche Scientifique (CNRS)
- 申请人地址： 1, quai de Tourville 44000 Nantes FR
- 专利权人： Université de Nantes,Chu Nantes,INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM),Centre National de la Recherche Scientifique (CNRS)
- 当前专利权人： Université de Nantes,Chu Nantes,INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM),Centre National de la Recherche Scientifique (CNRS)
- 当前专利权人地址： 1, quai de Tourville 44000 Nantes FR
- 代理机构： Ahner, Francis
- 优先权： FR0850018 20080103
- 国际公布： WO2009083613 20090709
- 主分类号： C07F9/38
- IPC分类号： C07F9/38
摘要：
The present invention relates to a method for preparing a hydroxy-bisphosphonic acid derivative or a salt thereof, from the corresponding carboxylic acid, comprising the following steps: - activation of the carboxylic acid function in the form of the boronate derivative thereof through the action of a borane, then - reaction with tris(trimethylsilyl)phosphite, under Arbuzov conditions - treatment with an alcohol, chosen in particular from an aliphatic alcohol or trifluoromethanol, and - separation of the hydroxy-bisphosphonic acid derivative formed, from the reaction medium.
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