Process for quinoline-3-carboxylic acid antibacterial agents

C - Chemistry – Metallurgy – 07 – D

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C07D 215/56 (2006.01) C07D 401/04 (2006.01) C07D 401/10 (2006.01) C07D 451/04 (2006.01) C07D 471/08 (2006.01) C07D 487/08 (2006.01)

Patent

CA 1283658

ABSTRACT An improved process for the preparation of 7- substituted amino-1-alkyl- or cyclopropyl-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1- cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxo- quinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product. The desired products have the general formula: Image wherein A is a substituted amino group and R2 is a C1-3alkvl or C3-6 cvcloalkyl.

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