Cesium carbonate → 4-(Azetidin-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 4-(azetidin-1-yl)-2-chloro-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (31 mg, 0.11 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (22.37 mg, 0.11 mmol), cesium carbonate (71.7 mg, 0.22 mmol), palladium(II) acetate (3.71 mg, 0.02 mmol) and 2-(dicyclohexylphosphino)biphenyl (5.79 mg, 0.02 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 minutes in microwave reactor. The mixture was filtered through a short silica plug which was washed with 10% methanol in ethyl acetate and the mixture was concentrated in vacuum. The residue was purified by preparative HPLC give the title compound as a dry film (41 mg, 83%).

Provenance & Evidence