PROCESS FOR THE PREPARATION OF 1-SUBST.-6-FLUORO-4-OXO-7- (1-PIPERAZINYL)-1,4-DIHYDROQUINOLINE-3-CARBOXYLIC ACID, NOVEL INTERMEDIATE FOR USE IN THIS PROCESS AND PROCESS FOR THE PREPARATION OF THIS INTERMEDIATE

A process for the preparation of 1-subst.-6-fluoro-4-oxo- 7-(1-piperazinyl)-1,4-dihydroquinoline-3-carboxylic acid II in which R1 is lower alkyl, lower cycloalkyl or 2,4-difluorophenyl is described, in which boron 1-subst.- 6-fluoro-4-oxo-7-(4-subst.-1-piperazinyl)-1,4- dihydroquinoline-3-carboxylat...

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Hauptverfasser: SKET BORIS DR, BARBO MARTIN, ZUPET PAVEL DR, ZUPANCIC NATASA DR
Format: Patent
Sprache:eng ; ger
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Zusammenfassung:A process for the preparation of 1-subst.-6-fluoro-4-oxo- 7-(1-piperazinyl)-1,4-dihydroquinoline-3-carboxylic acid II in which R1 is lower alkyl, lower cycloalkyl or 2,4-difluorophenyl is described, in which boron 1-subst.- 6-fluoro-4-oxo-7-(4-subst.-1-piperazinyl)-1,4- dihydroquinoline-3-carboxylate diacetate of the formula I is subjected to an alkaline hydrolysis. Compounds of the formula II are used in medicine for treating inflammatory disorders. The compound of the formula I is novel. It is obtained by nucleophilic substitution of the halogen atom in position 7 in boron 1-subst.-6-fluoro-4-oxo-7-halo-1,4- dihydroquinoline-3-carboxylate diacetate with 1-substituted piperazine.