- QUINOLINE DISULFIDES AS INTERMEDIATES
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A process for preparing rufloxacin using a compound of the formula I (I) as a starting material is described, where R is herein defined.
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- Process for the preparation of rufloxacin and salts thereof
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A process for the preparation of rufloxacin, a compound of the formula I STR1 and salts thereof is described. This is effected by reducing a quinoline disulfide of formula (II) as herein defined, and subjecting the resulting 2-mercaptoethyl quinoline of formula (III) as herein defined to a cyclization in a basic medium and hydrolyzing the rufloxacin ester thus obtained and, if desired, forming the salts thereof.
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- Quinilone disulfide as intermediates
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A process for preparing rufloxacin using a compound of the formula I STR1 as a starting material is described, where R is herein defined.
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- 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
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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.
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- 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
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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 H2 O and salification with HCl.
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- One-pot synthesis of rufloxacin
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Rufloxacin (MF-934) was prepared in one-pot synthesis in 61% yield by treatment of the 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)-benzoyl acetate, first with N,N-dimethylformamide dimethyl acetal, then with 2-aminoethanethiol, followed by cyclization and
- Cecchetti,Fravolini,Schiaffella
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p. 2301 - 2308
(2007/10/02)
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