发明名称 PRODUCTION OF QUINOLONECARBOXYLIC ACID DERIVATIVE
摘要 PURPOSE:To obtain the titled substance useful as an intermediate for synthesizing a compound useful as an antimicrobial agent simply in highyield, by using a novel aniline as a raw material, and subjecting the reaction product of the aniline and an alkoxymethylene malonic acid dialkyl ester to ring formation. CONSTITUTION:A novel compound shown by the formula [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., or R<4> and R<5> may be phthaloyl) is reacted with an alkoxymethylene malonic acid dialkyl ester or a mixtutre of an orthofomic ester and a malonic acid dialkyl ester under heating at 60-200 deg.C, preferably aat 100-160 deg.C. Then, the reaction product shown by the formula IV (R is lower alkyl) is subjected to ring formation, to give a compound shown by the formula V. The compound shown by the formula I is synthesized from a compound shown by the formula VI.
申请公布号 JPS61143364(A) 申请公布日期 1986.07.01
申请号 JP19840267138 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 A61K31/47;A61P31/04;C07D215/56 主分类号 A61K31/47
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