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1. 发明专利

JP2012036224A Process for synthesis of azetidinones 审中-公开
标题翻译：合成AZETIDINONES的方法
公开(公告)号：JP2012036224A
公开(公告)日：2012-02-23
申请号：JP2011252865
申请日：2011-11-18
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： THIRUVETTIPURAM THIRUVENGADAM K , CHIU JOHN S , FU XIAOYONG , MCALLISTER TIMOTHY L
IPC分类号： C07D205/08 , C07D201/02
CPC分类号： C07D205/08 , C07H17/02
摘要： PROBLEM TO BE SOLVED: To provide a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents.SOLUTION: The process includes reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent. The cyclizing agent is selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride.
摘要翻译：要解决的问题：提供一种制备可用作半乳聚糖和低胆固醇血症药的中间体的氮杂环丁酮的方法。解决方案：该方法包括使β-（取代氨基）酰胺，β-（取代氨基）酸酯或β-（取代氨基）硫代碳酸酯与甲硅烷基化剂和环化剂。环化剂选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵芳氧化物及其水合物，或其反应产物：（i）至少一种季铵卤化物和至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物。版权所有（C）2012，JPO＆INPIT

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