反应详情

温度

100 °C

A mixture of 3,5-dibromo-1-methylpyridin-2(1H)-one (2.67 g, 10.0 mmol), 6-aminopyridin-2-ol (1.1 g, 10.0 mmol), Pd2(dba)3 (460 mg, 0.5 mmol), Xantphos (576 mg, 1.0 mmol) and Cs2CO3 (6.52 g, 20.0 mmol) in DMF (40 mL) was stirred at 100° C. overnight. The mixture was concentrated and the residue was treated with DCM. The precipitate was collected by filtration and dried to give 5-bromo-3-(6-hydroxypyridin-2-ylamino)-1-methylpyridin-2(1H)-one 101a (4.0 g crude) as a brown solid.

1. concentrationThe mixture was concentrated
2. additionthe residue was treated with DCM
3. filtrationThe precipitate was collected by filtration
4. customdried