| 摘要 |
<p>Process for obtaining derivatives of 6-fluoro-1,4-dihydro-4-oxo-7-piperazynil-3-quinolinecarboxylic acid of formula (I) wherein R1 is H, linear or branched alkyl or hydroxyalkyl having from 1 to 4 carbon atoms and R2 is a linear or cyclic alkyl with 1 to 4 carbon atoms. The process consists in the reaction of a compound (VI) wherein R3 is a linear or branched alkyl with 1 to 5 carbon atoms and R1 may be additionally acyl or alkoxycarbonyl, with HNa and subsequent acid hydrolysis of the cyclic ester obtained. Some of the starting compounds (VI) are new, in particular 3-cyclopropylamino-2-2-chloro-5-fluoro-4-(4-ethoxycarbonyl-1-piperazynil)benzoylethylacrylate. Amongst the compounds (I) which may be obtained according to this process, cyprofloxazin, norfloxazin and enrofloxazin have the antibacterial activity which makes them appropriate in therapy.</p> |
