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

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-chloro-4-(4,4-difluoropiperidin-1-yl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (97 mg, 0.28 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (57 mg, 0.28 mmol), cesium carbonate (183 mg, 0.56 mmol), palladium acetate (9 mg, 0.04 mmol) and 2-(dicyclohexylphosphino)biphenyl (15 mg, 0.04 mmol) was stirred under argon at 120° C. for 90 minutes in a microwave reactor. The mixture was filtered through a short silica gel plug which was washed with 10% solution of methanol in ethyl acetate (75 mL). The eluate was concentrated in vacuum and the residue was purified by preparative HPLC to give the title compound as a gum, 103 mg (72%).

Provenance & Evidence