Process for preparing ciprofloxacine

C - Chemistry – Metallurgy – 07 – D

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C07D 401/10 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) C07D 215/00 (2006.01) C07D 215/56 (2006.01) C07D 295/00 (2006.01) C07D 401/04 (2006.01)

Patent

CA 1340561

The invention is concerned with a process for preparing ciprofloxacine of the formula (see fig.I) based on the reaction of 1-(2,4-dichloro-5-fluoro- phenyl)-1,3-butanedione with ethyl orthoformate, to give an enol ether which is reacted with cyclopropylamine, resulting in an enaminone, the cyclization of which provides a compound which is reacted with N-ethoxycar-bonylpiperazine, producing an intermediate, whose oxidation leads to an acid which provides ciprofloxacine by means of alkaline hydrolysis and neutralisation. Ciprofloxacine is a highly affective bactericidal agent against gram-positive and gram-negative bacteria.

602049

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