公开(公告)号：US5639878A

公开(公告)日：1997-06-17

申请号：US506052

申请日：1995-07-24

申请人： Chi Jang Moon ,  Kyung Up Baik ,  Sea Han Oh ,  Joon Wan Kim ,  Jae Ho Lee

发明人： Chi Jang Moon ,  Kyung Up Baik ,  Sea Han Oh ,  Joon Wan Kim ,  Jae Ho Lee

IPC分类号： C07B53/00 ,  C07D205/08 ,  C07F7/18 ,  C07B41/12

CPC分类号： C07D205/08 ,  C07F7/1892 ,  Y02P20/55

摘要： The present invention relates to a novel and improved process for preparing 4-acyloxy-2-azetidinone derivatives having the following formula (I) which are useful as an intermediate for synthesis of penem or carbapenem compounds: ##STR1## in which R.sub.1 represents a hydroxy-protecting group; and R.sub.3 represents an acyl group, which comprises reacting an azetidinone derivative having the following formula (II): ##STR2## wherein R.sub.1 is defined as above and R.sub.2 represents an alkyl group or an aryl group, with a N-haloacylimide in the presence of an organic carboxylic acid or a salt of an organic carboxylic acid.The present invention uses the organic compound, N-haloacylimide, as the reactant rather than the heavy metal reactant used in the prior art, and thus provides an economical advantage and does not cause any problem related to safety and waste disposal after the reaction.

摘要翻译： 本发明涉及一种制备具有下式（I）的4-酰氧基-2-氮杂环丁酮衍生物的新颖和改进的方法，其可用作青霉烯或碳青霉烯化合物的合成中间体：其中R1 表示羟基保护基; R 3表示酰基，其包括使具有下式（II）的氮杂环丁酮衍生物：其中R 1如上所定义，R 2表示烷基或芳基，与N-卤代酰亚胺在 存在有机羧酸或有机羧酸的盐。 本发明使用有机化合物N-卤代酰亚胺作为反应物，而不是现有技术中使用的重金属反应物，因此提供了经济的优点，并且不会引起任何与反应后的安全性和废物处理有关的问题。