7-isoindoline - manufacturing method of the quinolone carboxylic acid derivatives as well as manufacturing method of isoindoline-5-boronic acid derivative

摘要

PROBLEM TO BE SOLVED: To obtain the subject derivative useful as an antibacterial agent by reacting each specific isoindolineboronic acid derivative with a quinolonecarboxylic acid (salt) derivative in the presence of a metallic palladium, etc., in a good efficiency, in a high purity and in a high yield. ;SOLUTION: This 7-isoindoline-quinolonecarboxylic acid derivative of formula III is obtained by reacting an isoindoline-5-boronic acid derivative (salt) of formula I [R3 is H, a halogen (substituted) alkyl or the like; R4 is H, an aryl or the like; R5 is H, a (substituted) alkyl or the like; R7, R8 are each H, a lower alkyl and form a ring by bonding together] with a 7-eliminable group- substituted quinolonecarboxylic acid (salt) of formula II [R1 is H or a carboxy protecting group; R2 is a (substituted) alkyl or the like; R6 is H, a halogen or the like; A is CH or the like; X2 is an eliminable group] in the presence of a palladium (salt). Further, it is preferable to obtain a compound of formula VI by reacting a compound of formula IV (X1 is a halogen) with a dialkoxyborane of formula V (Z is an alkylene) or the like, and to react with a compound of formula II without isolating the compound of formula IV.;COPYRIGHT: (C)2000,JPO