Ethanol → HCID 18549176, compound

Participants

Reaction Conditions

Reaction Steps

Ethyl 1-(2,4-difluorophenyl)-7-fluoro-8-[4-(4-fluorophenyl)piperazin-1-yl]-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine-3-carboxylate was obtained under the conditions of Example 13, but from 3.68 g of ethyl 3-(2-chloro-6,7-difluoro-3-quinolyl)-2-dimethylaminomethylene-3-oxopropionate and 3.87 g of 2,4-difluoroaniline in 40 cm3 of trichloromethane. 50 cm3 of ethanol and 1.5 cm3 of 1,8-diazabicyclo[5.4.0]undec-7-ene were added to the mixture, which was heated at a temperature around 80° C. for approximately 1 hour. After cooling to a temperature around 10° C., the product was filtered off and washed 2 times with 50 cm3 of ethanol and 2 times with 50 cm3 of isopropyl ether. 3.3 g of ethyl 1-(2,4-difluorophenyl)-7,8-difluoro-4-oxo-1,4-dihydro-benzo[b][1,8]naphthyridine-3-carboxylate were obtained in the form of a yellow solid melting at approximately 300° C., which solid was used without additional purification in the subsequent stages.

Provenance & Evidence