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) of formula (I) by reaction of 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl ethyl acetate of formula (II) with N,N-dimethylformamide dimethylacetal, followed by reaction with 2-aminoethanethiol, intramolecular cyclization by treatment with NaH, hydrolysis with H₂O and salification with HCl.
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
CECCHETTI, Violetta;FRAVOLINI, Arnaldo;SCHIAFFELLA, Fausto
1992
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) of formula (I) by reaction of 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl ethyl acetate of formula (II) with N,N-dimethylformamide dimethylacetal, followed by reaction with 2-aminoethanethiol, intramolecular cyclization by treatment with NaH, hydrolysis with H₂O and salification with HCl.File in questo prodotto:
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