Cesium carbonate → 4-(1-Ethoxyvinyl)-N-(3-methoxy-4-(2-methyloxazol-5-yl)phenyl)-6-((2,2,2-trifluoroethoxy)-methyl)pyrimidin-2-amine

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Reaction Conditions

Reaction Steps

2-Chloro-4-(1-ethoxyvinyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (0.10 g, 0.34 mmol) was dissolved in dioxane (5 mL). 3-Methoxy-4-(2-methyloxazol-5-yl)aniline (0.069 g, 0.34 mmol), cesium carbonate (0.220 g, 0.67 mmol), palladium(II) acetate (0.011 g, 0.05 mmol) and 2-(dicyclohexylphosphino)biphenyl (0.018 g, 0.05 mmol) were added. The vial was capped, evacuated and flushed with nitrogen. The mixture was heated by microwave irradiation at 120° C. for 1.5 h. The solvents were evaporated. EtOAc was added and the mixture was filtered through a plug of silica. The solvents were evaporated and the residue was purified by column chromatography on silica eluting with EtAOc to give the title compound as a solid, 138 mg (88%).

Provenance & Evidence