Dimethyl Sulfoxide → HCID 10167035, compound

Participants

Reaction Conditions

Reaction Steps

A mixture consisting of 5-amino-6,7-difluoro-1-[(1R,2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid (0.33 g, 1.06 mmol), (3S,4R)-4-(1-tert-butoxycarbonylaminocyclopropyl)-3-fluoro pyrrolidine (0.39 g, 1.60 mmol), 1-methylpiperidine (0.16 ml, 1.33 mmol) and dimethyl sulfoxide (13 ml) was heated at an outer temperature of 80° C. for 7 hours under a condition of 2.94×108 Pa. When analysis was carried out by a high performance liquid chromatography after completion of the reaction, formed ratio of the compound of interest 5-acetylamino-7-[(3S,4R)-4-(1-tert-butoxycarbonylaminocyclopropyl)-3-fluoropyrrolidinyl]-6-fluoro-1-[(1R,2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid was 17%. Also, residual ratio of the starting material was 79%.

Provenance & Evidence