公开(公告)号：US20120083601A1

公开(公告)日：2012-04-05

申请号：US13323366

申请日：2011-12-12

申请人： TIRUVETTIPURAM K. THIRUVENGADAM ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

发明人： TIRUVETTIPURAM K. THIRUVENGADAM ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

IPC分类号： C07D205/08

CPC分类号： C07D205/08 ,  C07H17/02

摘要： A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising 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 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, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

摘要翻译： 提供了一种制备氮杂环丁酮的方法，所述氮杂环丁酮可用作半乳聚糖和低胆固醇血症药物的合成中的中间体，包括使（b） - （取代的 - 氨基）酰胺，和（取代的 - 氨基）酸酯， （取代 - 氨基）硫代碳酸酯与甲硅烷基化剂和选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵氧化物及其水合物的环化剂或其反应产物 ：（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，其中环化剂的季铵部分是未取代的或被一至四个独立地选自 由烷基，芳烷基和芳基烷基 - 烷基组成。