Cesium carbonate → 4-(Azetidin-1-yl)-N-(3-methoxy-4-(6-methylpyridazin-4-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 (30 mg, 0.11 mmol), 3-methoxy-4-(6-methylpyridazin-4-yl)aniline (23 mg, 0.11 mmol), cesium carbonate (69 mg, 0.21 mmol), palladium(II) acetate (4 mg, 0.02 mmol) and 2-(dicyclohexyl-phosphino)biphenyl (6 mg, 0.02 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 minutes in a microwave reactor. The mixture was filtered through a short silica plug which was washed with 10% solution of methanol in EtOAc (75 mL). The eluate was concentrated and the residue was purified by preparative HPLC to give the title compound as a solid 14 mg (29%).

Provenance & Evidence