Cesium carbonate → 4-(1-Ethoxyvinyl)-N-(3-methoxy-4-(4-methoxy-1H-imidazol-1-yl)phenyl)-6-((2,2,2-trifluoro-ethoxy)methyl)pyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

2-Chloro-4-(1-ethoxyvinyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (0.230 g, 0.78 mmol), 3-methoxy-4-(4-methoxy-1H-imidazol-1-yl)aniline, palladium(II) acetate (0.026 g, 0.12 mmol), 2-(dicyclohexylphosphino)biphenyl (0.041 g, 0.12 mmol), cesium carbonate (0.505 g, 1.55 mmol) and dioxane (20 mL) were mixed in a vial. The vial was capped, evacuated and flushed with nitrogen. The mixture was heated by microwave irradiation at 120° C. for 1.5 h. The mixture was filtrated through pad of silica and silica was washed by EtOAc containing 10% of MeOH. The solvents were evaporated and the residue was purified by column chromatography eluting with gradient of MeOH and DCM to give the title compound as a dry film, 0.313 g (84%).

Provenance & Evidence