反应详情

A solution of 8.3 g of 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, 7.1 g of 2 -(methylaminomethyl)morpholine dihydrochloride and 15.2 g of 1,8-diazabicyclo[5.4.0]undec-7-ene in 166 ml of acetonitrile is refluxed for 8 hours. After ice-cooling, the precipitated crystals are collected by filtration, washed with acetone and recrystallized from dimethylformamide to give 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[2-(methylaminomethyl)-morpholino]-4-oxoquinoline-3-carboxylic acid, melting at 257°-259° C. with decomposition. The corresponding hydrochloride melts at 288°-290° C. with decomposition.

1. temperatureAfter ice-cooling
2. filtrationthe precipitated crystals are collected by filtration
3. washwashed with acetone
4. customrecrystallized from dimethylformamide