Fremgangsmate for fremstilling av 7-isoindolinkinolonkarboksylsyre-derivater og mellomprodukter for disse, salter av 7-isoindolinkinolonkarboksylsyrer, hydrater derav, og

摘要

This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula Ä1Ü which is useful as an antibacterial agent, and an intermediate thereof: wherein R<1> represents a hydrogen atom or a carboxyl-protecting group; R<2> represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R<3> represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R<4> represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R<4> bonds; R<5> represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R<6> represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C-R<7> in which R<7> represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by the general formula Ä1Ü, a hydrate thereof and a composition comprising them as an active ingredient.