反应详情

BBr3 (20 mL) was added dropwise to a mixture of compound 5-bromo-N-(4-fluorobenzyl)-2-methoxynicotinamide (2.0 g, 5.9 mmol) in DCM (10 mL) at −78° C. The mixture was stirred at RT for 10 h, and then MeOH (20 mL) was added to quench the reaction. The mixture was concentrated in vacuum to give the product of 5-bromo-N-(4-fluorobenzyl)-2-hydroxynicotinamide (1.8 g, yield: 95%). 1H-NMR (DMSO-d6, 400 MHz) δ 12.9 (s, 1H), 10.0 (t, J=4.8 Hz, 1H), 8.30 (d, J=2.8 Hz, 1H), 8.02 (s, 1H), 7.34 (dd, J=6.0, 8.8 Hz, 2H), 7.15 (d, J=8.8 Hz, 2H), 4.50 (s, 2H). MS (M+H)+: 325/327

1. customto quench
2. customthe reaction
3. concentrationThe mixture was concentrated in vacuum