发明名称 Process for the preparation of derivatives of beta-lactam antibiotics
摘要 beta -lactam antibiotics of the formula <IMAGE> in particular cephamycin and cephalosporin derivatives, are prepared by reacting a compound of the formula <IMAGE> with an acyl halide of the formula R<1>-Y in the presence of a halogenated aliphatic hydrocarbon solvent, forming a compound of the formula <IMAGE> The phenacyl or halophenacyl protective group is then removed by reaction with zinc and an acid. The acid is selected from inorganic acids, mono-esters of dibasic inorganic acids and sulphonic acids. The resulting compound of the formula I can then be converted into a pharmaceutically acceptable salt. In this way, compounds can be obtained in a high yield with a minimum of secondary reactions. In the formulae, R<1>, R<2>, R<3>, R<4>, R<5>, X and Y have the definitions given in Patent Claim 1.
申请公布号 CH646977(A5) 申请公布日期 1984.12.28
申请号 CH19820001082 申请日期 1982.02.22
申请人 SANKYO CO. LTD. 发明人 JUNICHI, NAKAZAWA;MASANAO, KANEKO;TAKEO, MIYAOKA
分类号 A61K31/395;C07D;C07D471/04;C07D498/04;C07D501/04;C07D501/20;C07D501/36;C07D501/57;(IPC1-7):C07D501/57 主分类号 A61K31/395
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