发明名称 PRODUCTION OF QUINOLONECARBOXYLIC ACID DERIVATIVE
摘要 PURPOSE:To obtain the titled substance useful as an intermediate for synthesiz ing a compound useful as an antimicrobial agent simply in high yield, by using an aniline as a raw material, reacting it with an alkoxymethylene malonic acid dialkyl ester, etc., and denitrating and subjecting the reaction product to ring formation simultaneously. CONSTITUTION:A compound shown by the formula I (X and Y are halogen; Z is group shown by the formula II, or formula III; R<1> and R<2> are H, or lower alkyl; R<3> is H, lower alkyl, lower acyl, lower alkoxycarbonyl, etc.; R<4> is H, lower alkyl, etc.; R<5> is H, lower alkyl, etc.) is reacted with an alkoxymethylene malonic acid dialkyl ester or a mixture of a orthoformic ester and a malonic acid dialkyl ester, to give a compound shown by the formula IV (R is lower alkyl). Then, this compound is heated in the presence of a catalyst, denitrated and sumultaneously subjected to ring formation to give a compound shown by the formula V. The compound shown by the formula I is a novel compound, and it is synthesized from a compound shown by the formula VI as a starting raw material through several processes.
申请公布号 JPS61143363(A) 申请公布日期 1986.07.01
申请号 JP19840267137 申请日期 1984.12.17
申请人 KYORIN PHARMACEUT CO LTD 发明人 IRIKURA TSUTOMU;SUZUE SEIGO;ISHIZAKI TAKAYOSHI
分类号 C07D401/04;A61K31/47;A61K31/495;A61P31/04;C07D215/00;C07D215/56;C07D241/00 主分类号 C07D401/04
代理机构 代理人
主权项
地址