反应详情

To a mixture of 3-(3-fluorophenoxy)azetidine) (D50) (106.73 mg, 0.638 mmol) and triethylamine (0.11 ml, 0.798 mmol) in methanol (3 ml), 2-Chloro-5-(trifluoromethyl)nicotinic acid (120 mg, 0.532 mmol) was added and the mixture was heated 10 min (2 cycles of 5 min each) under microwave irradiation at 150° C. After solvent evaporation the residue was purified by SPE-Si cartridge (25 g) eluting with a mixture dichloromethane/methanol from 100/0 to 50/50. Collected fraction after solvent evaporation afforded the title compound (D121) (83 mg)

1. additionwas added
2. temperaturethe mixture was heated 10 min (2 cycles of 5 min each)
3. customunder microwave irradiation at 150° C
4. customAfter solvent evaporation the residue
5. customwas purified by SPE-Si cartridge (25 g)
6. washeluting with a mixture dichloromethane/methanol from 100/0 to 50/50
7. customCollected fraction
8. customafter solvent evaporation