Cesium carbonate → 4-((Cyclopropylmethoxy)methyl)-6-(1-ethoxyvinyl)-N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)pyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-chloro-4-((cyclopropylmethoxy)methyl)-6-(1-ethoxyvinyl)pyrimidine (88 mg, 0.33 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (67 mg, 0.33 mmol), cesium carbonate (213 mg, 0.65 mmol), palladium acetate (11 mg, 0.05 mmol) and 2-(dicyclohexylphosphino)biphenyl (17 mg, 0.05 mmol) in dioxane (2 mL) were heated under argon atmosphere at 120° C. for 90 minutes in microwave reactor. The mixture was filtered through a short silica plug which was washed with 10% MeOH in EtOAc. The solvents were evaporated and the residue was purified by preparative to give the title compound 98 mg (69%).

Provenance & Evidence