反应详情

8.0 g of ethyl 3-(2-fluoroethylamino)-2-(2,3,4,5-tetrafluorobenzoyl)acrylate was dissolved in 64 ml of acetonitrile under heating to 75˜80° C. 9.06 g (1.8 eq.) of K3PO4 was added in portions to the reaction mixture, which was then stirred at the same temperature for 1.5 hours. The reaction mixture was filtered under a reduced pressure and washed with 80 ml of dichloromethane. The filtrate was concentrated under a reduced pressure. The resulting residue was dissolved in 48 ml of dichloromethane and then washed with water. The organic layer was concentrated under a reduced pressure to give 7.29 g of ethyl 6,7,8-trifluoro-1-(2-fluoroethyl)-1,4-dihydro-4-oxoquinoline-3-carboxylate (Yield: 96.9%).

1. temperatureunder heating to 75˜80° C
2. filtrationThe reaction mixture was filtered under a reduced pressure
3. washwashed with 80 ml of dichloromethane
4. concentrationThe filtrate was concentrated under a reduced pressure
5. dissolutionThe resulting residue was dissolved in 48 ml of dichloromethane
6. washwashed with water
7. concentrationThe organic layer was concentrated under a reduced pressure