PROCESSES FOR PRODUCING 7-ISOINDOLINEQUINOLONECARBOXYLIC ACID DERIVATIVES AND INTERMEDIATES THEREFOR,SALTS OF 7-ISOINDOLINEQUINOLONECARBOXYLIC ACIDS, HYDRATES THEREOF, AND COMPOSITIONS CONTAINING THE SAME AS ACTIVE INGREDIENT.

摘要

This invention relates to processes for producinga 7-isoindoline-quinolonecarboxylic acid derivativerepresented by the general formula [1] which is useful asan antibacterial agent, and an intermediate thereof:wherein R1 represents a hydrogen atom or a carboxyl-protecting group; R2 represents a substituted orunsubstituted alkyl, alkenyl, cycloalkyl, aryl orheterocyclic group; R3 represents at least one groupselected from hydrogen atom, halogen atoms, substituted orunsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy oralkylthio groups, nitro group, cyano group, acyl groups,protected or unprotected hydroxyl groups and protected orunprotected or substituted or unsubstituted amino groups; R4represents 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 unsubstitutedamino groups, alkylidene groups, oxo group and groups eachforming a cycloalkane group together with the carbon atomto which R4 bonds; R5 represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl,cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or arylgroup; R6 represents a hydrogen atom, a halogen atom, asubstituted or unsubstituted alkyl, alkoxy or alkylthiogroup, a protected or unprotected hydroxyl or amino groupor a nitro group; and A represents CH or C-R7 in which R7represents a halogen atom, a substituted or unsubstitutedalkyl, alkoxy or alkylthio group or a protected orunprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by thegeneral formula [1], a hydrate thereof and a compositioncomprising them as an active ingredient.