PROCESS FOR THE PREPARATION OF 1-METHYLAMINO- QUINOLINE-CARBOXYLIC ACID DERIVATIVES

摘要

The present invention relates to a process for the preparation of compounds of the general Formula I /I/ and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II /II/ (wherein R1 and R2 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms) with a piperazine of the general Formula III /III/ (wherein R3 represents hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general formula IV /IV/ thus obtained (wherein R, R1 and R2 are as stated above) without or after hydrolysis and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the general Formula I are known antibacterial agents. The advantage of the process of the present invention is that it enables the preparation of the compounds of the general formula I in a simple manner, with high yields and in a short reaction time.