Process for the preparation of 9-fluoro-10-(4-methyl-1-piperazin

Details Process for the preparation of 9-fluoro-10-(4-methyl-1-piperazin Process for the preparation of 9-fluoro-10-(4-methyl-1-piperazin

1992-05-29

1993-06-22

Ford, John M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D51304

Patent

active

052217418

ABSTRACT:
Process for the preparation of 9-fluoro-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acid hydrochloride (Rufloxacin) by reaction of 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl ethyl acetate with N,N-dimethylformamide dimethylacetal, followed by reaction with 2-aminoethanethiol, intramolecular cyclization by treatment with NaH, hydrolysis with H.sub.2 O and salification with HCl.

REFERENCES:
patent: 4668784 (1987-05-01), Mascellani et al.
Chemical Abstracts, vol. 108, No. 19, May 9, 1988; p. 654, Abstract No. 167489b, Columbus, OH, US & JP-A-62 216 591 (Dainippon Pharmaceutical Co., Ltd.) Sep. 22, 1987.
Synthetic Communications, vol. 21, N. 22, 1991; pp. 2301-2308, Marcel Dekker, Inc., New York, US; V. Cecchetti et al.: "One-pot synthesis of rufloxacin".
Cecchetti et al.; "Quinolonecarboxylic Acids. 2. Synthesis and Antibacterial Evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids"; J. Med. Chem., 1987, 30, 465.
Drugs of the Future, vol. 15, No. 7, 1990, pp. 762-767.

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