Highly soluble antibacterially active organic salts of pyridoben

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544 32, A61K 3154, C07D51304

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active

049101960

ABSTRACT:
New highly soluble antibacterially active salts of pyridobenzothiazines with organic acids are described.
In particular, organic salts of 9-fluoro-10[N-(4'-methyl)piperazinyl]-7-oxo-2,3-dihydro-7H-pyrido[1,2,3][1 ,4]-benzothiazine-6-carboxylic acid are prepared with an acid chosen from the group consisting of methanesulphonic acid, ethanesulphonic acid, n-dodecanesulphonic acid, p-toluenesulphonic acid, 1-actadecanesulphonic acid, 2-chloro-ethanesulphonic acid, 2-bromo-ethanesulphonic acid, 3-hydroxy-propanesulphonic acid, citric acid, malonic acid, gluconic acid, malic acid, lactic acid and L-tartaric acid.
A new process is also described for preparing said salts from 2,3,4-trichloronitrobenzene, by way of a 2-fluoro-3-chloro-4-mercapto derivative of the nitrobenzene and cyclizing the corresponding amino derivative.

REFERENCES:
patent: 4668784 (1987-05-01), Mascellani et al.
Mediolanum Farmaceutiti, Chemical Abstracts, vol. 104:207290f (1986).
Otsuka Pharm., Chemical Abstracts, vol. 101:151868u (1984).
Daiichi Seiyaku, Chemical Abstracts, vol. 98:198294p (1983).
Fravolini et al., Chemical Abstracts, vol. 105:218250q (1985).
Cecchetti et al., Chemical Abstracts, vol. 106:102,235e (1987).

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