Cesium carbonate → 1-(2-(3-Methoxy-4-(4-methyl-1H-imidazol-1-yl)phenylamino)-6-((2,2,2-trifluoroethoxy)-methyl)pyrimidin-4-ylamino)-2-methylpropan-2-ol

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (45 mg, 0.22 mmol), 1-(2-chloro-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-ylamino)-2-methylpropan-2-ol (35 mg, 0.11 mmol), cesium carbonate (73 mg, 0.22 mmol), palladium(II) acetate (4 mg, 0.02 mmol) and 2-(dicyclohexylphosphino)biphenyl (6 mg, 0.02 mmol) in dioxane (1 mL) was heated at 120° C. by microwave irradiation under nitrogen atmosphere for 90 minutes. An additional equivalent of each: 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline, cesium carbonate, palladium(II) acetate and 2-(dicyclohexylphosphino)biphenyl was added and the reaction mixture was heated by microwave irradiation at 120° C. for additional 90 minutes. The mixture was filtered and purified by preparative HPLC to give the title compound as a solid 16 mg (29%).

Provenance & Evidence