反应详情

温度

80 °C

To a mixture of 2-(azetidin-3-yloxy)-5-fluoropyrimidine (D51) (108 mg, 0.638 mmol) and triethylamine (0.11 ml, 0.798 mmol) in methanol (1 ml) and tetrahydrofuran (2 ml), 2-chloro-5-(trifluoromethyl)nicotinic acid (120 mg, 0.532 mmol) was added and the mixture was heated 2 h at 80° C. After solvent evaporation the residue was purified by SPE-Si cartridge (25 g) eluting with a mixture dichloromethane/methanol from 95/5 to 80/20. Collected fraction after solvent evaporation afforded the title compound (D131) (44 mg)

1. additionwas added
2. customAfter solvent evaporation the residue
3. customwas purified by SPE-Si cartridge (25 g)
4. washeluting with a mixture dichloromethane/methanol from 95/5 to 80/20
5. customCollected fraction
6. customafter solvent evaporation