反应详情

温度

100 °C

A degassed mixture of 4-morpholin-4-yl-2-nitro-phenylamine (290 g, 1.3 mmol), 1-(6-chloro-pyrimidin-4-yl)-3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-methyl-3-(2-trimethylsilanyl-ethoxymethyl)-urea (Procedure 2E, step b; 624 g, 1.2 mmol), Pd2(dba)3 (110 g, 0.12 mmol), Xantphos (139 g, 0.24 mmol) and Cs2CO3 (782 g, 2.4 mmol) in toluene (15 mL) was heated at 100° C. for 2.5 hours. The reaction was concentrated, and the residue was purified by chromatography flash on silica to obtain the title compound (440 mg, yield: 49%) as a red solid. MS (ESI): 708 [M+H]+.

1. concentrationThe reaction was concentrated
2. customthe residue was purified by chromatography flash on silica