Hydrochloric Acid → Olamufloxacin

Participants

Reaction Steps

A 20% sodium hydroxide aqueous solution (4.8 ml) was added to 76.7% purity 5-acetylamino-7-[(7S)-7-tert-butoxycarbonylamino-5-azaspiro[2.4]hept-5-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid (400.1 mg) under stirring at room temperature, and the mixture was stirred at 80° C. for 5 hours. While stirring at room temperature, the reaction solution was mixed with concentrated hydrochloric acid and stirred for 1 hour. When quantitative analysis was carried out by a high performance liquid chromatography after neutralization of the reaction solution by adding 20% sodium hydroxide aqueous solution, formed amount of the compound of interest 5-amino-7-[(7S)-7-amino-5-azaspiro[2.4]hept-5-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid corresponded to 207.2 mg. The formation ratio was 92%.

Provenance & Evidence