PROCESS FOR PRODUCING QUINOLONECARBOXYLIC ACID DERIVATIVE.

摘要

A process for producing a 6-fluoro-7-substituted quinolonecarboxylic acid derivative represented by general formula (4) (wherein R1 represents alkyl; R2 represents hydrogen, halogen or alkoxy; X represents -CH2-, -NR4- or -O-; R4 represents hydrogen or alkyl; Y represents hydrogen, amino or alkylamino; and n represents 0 or 1), characterized by conducting thermal condensation of a 6-fluoroquinolonecarboxylic acid derivative represented by general formula (1) (wherein R1 and R2 are as defined above; and R3 represents a group capable of nucleophilic substitution), with a substituted saturated heterocyclic amine represented by general formula (2) (wherein X, Y and n are as defined above; and R4 represents hydrogen or alkyl), in the presence of an alkyl borate represented by the general formula (3): B(OR5)3 wherein R5 represents alkyl, etc. <CHEM>