反应详情

31.2 g of potassium hydrogensulphate are added at room temperature to a suspension of 46 g of ethyl 2-ethoxy-4,5-dihydro-4-oxofuran-3-carboxylate and 39.3 g of N-[(6-chloropyridin-3-yl)methyl]-2,2-difluoroethylamine in 705 ml of butyronitrile. The mixture was heated to reflux for 5 hours. Subsequently, it was cooled to room temperature and washed with 890 ml of water. The solvent was removed under reduced pressure. This gave 51 g of 4-[[(6-chloropyridin-3-yl)methyl](2,2-difluoroethyl)amino]furan-2(5H)-one (this corresponds to a 93% yield).

1. temperatureThe mixture was heated
2. temperatureto reflux for 5 hours
3. washwashed with 890 ml of water
4. customThe solvent was removed under reduced pressure