One-pot process for the preparation of 3-quinolonecarboxylic...

C - Chemistry – Metallurgy – 07 – D

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C07D 498/04 (2006.01) C07D 215/56 (2006.01) C07D 401/04 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2137523

The present invention relates to a one-pot process for the preparation of 7-heterocyclyl-substituted 3-quinolonecarboxylic acid derivatives of general formula (Ia). They possess a strong anti-microbial effect. They include active compounds such as, for example, ofloxacin, ciprofloxacin or enrofloxacin. (see Formula Ia) wherein: R' and R", together with the nitrogen atom to which they are bonded, form a monocyclic or bicyclic heterocycle which optionally contain further nitrogen, oxygen or sulphur hetero atoms, and which are optionally substituted; A represents CH, CF, CCl, C-OCH3 or C-CH3; X1 represents H, a halogen atom, NH2 or CH3; and R1 represents: (i) C1-C3-alkyl or FCH2CH2-, or (ii) cyclopropyl or phenyl which are optionally substituted once to three times by a halogen atom.

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