Process for the preparation of quinoline carboxylic acid...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) C07D 215/56 (2006.01) C07F 5/02 (2006.01)

Patent

CA 1325010

A B S T R A C T The invention relates to a new process for the preperation of compounds of the general Formula I Image (I) (wherein R1 stands for phenyl being optionally substituted by 1 or 2 halogen atoms, or a group of the general Formula - CH2CR6R7R8 (wherein R6, R7 and R8 stand for hydrogen or halogen); R2 stands for piperazinyl or 4-methyl-piperazinyl; R3 stands for hydrogen or fluorine) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II Image (II) (wherein R stands for halogen or an aliphatic acyloxy group containing 2 to 6 carbon atoms or an aromatic acyloxy group containing 7 to 11 carbon atoms, R4 stands for fluorine or chlorine with a piperazine derivative of the general Formula III Image (III) (wherein R5 stands for hydrogen or methyl) or a salt thereof and subjecting the compound of the general Formula IV Image (IV) thus obtained (wherein R, R1, R2 and R3 are as stated above) to hydrolysis after or without isolation and if desired con- verting 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 makes the desired compounds of the general Formula I available in a simple manner, with high yields and in a short reaction time.

570183

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