Cesium carbonate → N2-(3-Methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-N4-(oxetan-3-yl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine-2,4-diamine

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (78 mg, 0.38 mmol), 2-chloro-N-(oxetan-3-yl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-amine (57 mg, 0.19 mmol), cesium carbonate (125 mg, 0.38 mmol), palladium(II) acetate (6.45 mg, 0.03 mmol) and 2-(dicyclohexylphosphino)biphenyl (10.07 mg, 0.03 mmol) in dioxane (1 mL) was heated at 120° C. by microwave irradiation under nitrogen atmosphere for 90 minutes. The mixture was filtered through diatomeous earth and the filter pad was washed with methanol. The eluate was concentrated in vacuum and purified by preparative chromatography yielding the title compound as a solid 45 mg (51%).

Provenance & Evidence