METHOD FOR PREPARING AZETIDINONE COMPOUND AND INTERMEDIATE OF AZETIDINONE COMPOUND
申请人:Zhejiang Hisun Pharmaceutical Co., Ltd.
公开号:EP3153496A1
公开(公告)日:2017-04-12
Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
本发明公开了一种制备式 (I) 所代表的氮杂环丁酮化合物的新方法。以式(II)代表的羧基酮酯为原料,经过格氏加成、立体选择性脱水、酯基还原、羟基保护、与手性助剂缩合后与亚胺加成、环化和脱保护得到式(I)代表的化合物。本发明具有原料易得、合成步骤少、操作简单、收率高、立体选择性好、成本低等优点,可用于工业生产。