发明授权
US5221741A Process for the preparation of 9-fluoro-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-d e][1,4]benzothiazine-6-carboxylic acid hydrochloride 失效
9-氟代-10-(4-甲基-1-哌啶子基)-7-氧代-2,3-二氢-7H-吡啶并[1,2-a](1,4)苯并噻嗪 - 6-羧酸氢氯化物

Process for the preparation of
9-fluoro-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-d
e][1,4]benzothiazine-6-carboxylic acid hydrochloride
摘要:
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.
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