反应详情

3-(Benzyloxy)-5-bromo-1-(propan-2-yl)pyridin-2(1H)-one (58 mg, 0.180 mmol), 4-chloro-3-(trifluoromethyl)phenylboronic acid (49 mg, 0.218 mmol), and Pd(dppf)Cl2—CH2Cl2 (8 mg, 9.80 μmol) were combined in THF (1 mL) in a microwave vessel. To this was added 1 M Cs2CO3 (0.540 mL, 0.540 mmol). The vessel was sealed then irradiated to 150° C. for 20 min. The layers were separated and the aqueous extracted with EtOAc (3×). The combined organic layers were filtered through a pad of silica gel washing with EtOAc. The filtrate was concentrated to give 3-(benzyloxy)-5-[4-chloro-3-(trifluoromethyl)phenyl]-1-(propan-2-yl)pyridin-2(1H)-one (86 mg) which was used directly in the next step without purification.

1. customThe vessel was sealed
2. customthen irradiated to 150° C. for 20 min
3. customThe layers were separated
4. extractionthe aqueous extracted with EtOAc (3×)
5. filtrationThe combined organic layers were filtered through a pad of silica gel washing with EtOAc
6. concentrationThe filtrate was concentrated