NOVEL QUINOLONE DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THE SAME

摘要

NEW MATERIAL:The compound of formula I [R<1> is H or carboxy-protecting group; R<2> is H, halogen, hydroxy, lower alkoxy, etc.; A is O, S or N-R<3> (R<3> is H or amino-protecting group); X is H or halogen; Y is N or C-R<4> (R<4> is H, halogen, lower alkyl, etc.); Z is halogen or N-containing heterocyclic group)]. EXAMPLE:3-(Oxetan-3-yl-amino)-2-(2,3,4,5-tetrafluorobenzoyl)acrylic acid ethyl ester. USE:An antibacterial agent exhibiting excellent antibacterial activity against Gram-negative bacteria and Gram-positive bacteria. PREPARATION:The objective compound of formula I wherein R<1> is H or lower alkyl can be produced by reacting a compound of formula II (X<1> and X<2> are halogen; R<1a> is lower alkyl) with an orthoformic acid ester and then with a compound of formula III and subjecting the resultant compound of formula IV to cyclization reaction and hydrolysis.