反应详情

温度

90 °C

To a mixture of compound (4) (3.5 g, 13.5 mmol), pyridine-4-yl-boronic acid (4.9 g, 40.4 mmol), Pd(dppf)Cl2 (1.1 g, 1.3 mmol) and Cs2CO3 (13.1 g, 40.4 mmol) in DME/water (4/1, 80 ml) was stirred at 90° C. overnight. The solution was concentrated and purified by column chromatography on silica gel (DCM/MeOH=100:1) to give title compound as off-white solid (1.6 g, 40%). LC-MS (ESI+): m/e 303 (M+H)+, Rt: 0.561 min.

1. concentrationThe solution was concentrated
2. custompurified by column chromatography on silica gel (DCM/MeOH=100:1)