C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) A61K 31/33 (2006.01) A61K 47/12 (2006.01) C07C 63/64 (2006.01) C07D 215/02 (2006.01) C07D 215/12 (2006.01) C07D 215/233 (2006.01) C07D 215/56 (2006.01) C07D 295/02 (2006.01) C07D 295/04 (2006.01) C07D 295/073 (2006.01) C07D 295/14 (2006.01) C07D 401/10 (2006.01) C07D 403/04 (2006.01) C07F 5/00 (2006.01) C07F 5/02 (2006.01) C07F 5/04 (2006.01)
Patent
CA 2111181
12 ABSTRACT Disclosed is a process for preparing 1-substituted-6-fluoro-4-oxo-7-(1-piperazinyl)- 1,4-dihydroquinoline-3-carboxylic acid of the formula II Image II wherein R1 represents a lower alkyl, a lower cycloalkyl or 2,4-difluorophenyl, wherein 1-substituted-6-fluoro-4-oxo-7-(4-substituted-1-piperazinyl)-1,4-dihydro- quinoline-3-carboxylate boron diacetate of the formula I Image I wherein R2 represents a lower alkyl, or an optionally substituted phenyl, is subjected to an alkaline hydrolysis. Compounds of the forrnula II are used in medicine for the treatment of inflammatory diseases. The compound of the formula I is novel. It is obtained by a nucleophilic substitution of the halo atom in 7-position in the compound of the formula III Image III 13 with 1-substituted piperazine of the formula Image
Barbo Martin
Sket Boris
Zupancic Natasa
Zupet Pavel
Borden Ladner Gervais Llp
P.o. Krka Tovarna Zdravil
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