发明名称 AZETIDINONE COMPOUND AND ITS PRODUCTION
摘要 PURPOSE:To obtain the subject new compound, having excellent pharmacological action such as anti-inflammatory, analgesic, blood platelet agglutination inhibitory actions, etc., and useful as analgesic and antiphlogistic agents, agents for circulatory organs, etc., and useful as an intermediate for antibiotic substances such as cabapenem. CONSTITUTION:A compound expressed by formula I (R<1> and R<2> are H, alkyl, etc.; R<3> is H, aryl, etc.) or its salt, e.g. 4-difluoromethyl-1-(4-methoxyphenyl)-2- azetidinone. The above-mentioned compound is obtained by reacting a difluoroethaneimine compound expressed by formula II with a compound expressed by formula III (R<1>' and R<2>' are H, alkyl, etc., having protected OH; R<4> is alkyl) and then eliminating the protecting groups of OH groups from the product. The compound expressed by formula II is preferably reacted with a compound expressed by formula III in a solvent such as THF at -78 to 0 deg.C for 1-10hr while being stirred. Furthermore, the compound expressed by formula II is preferably obtained by reacting a difluoroacetaldehyde alkylhemiacetal with a primary amine expressed by the formula R<3>-NH2.
申请公布号 JPH0558993(A) 申请公布日期 1993.03.09
申请号 JP19910246759 申请日期 1991.08.30
申请人 YOSHITOMI PHARMACEUT IND LTD 发明人 KITATSUME TOMOYA
分类号 A61K31/395;A61K31/397;A61P7/02;A61P9/00;A61P25/04;A61P29/00;C07D205/08 主分类号 A61K31/395
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