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

関与物質

反応条件

反応手順

A mixture of 2-chloro-4-(4,4-difluoropiperidin-1-yl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (40 mg, 0.12 mmol), 3-methoxy-4-(6-methylpyridazin-4-yl)aniline (25 mg, 0.12 mmol), cesium carbonate (75 mg, 0.23 mmol), palladium(II) acetate (4 mg, 0.02 mmol) and 2-(dicyclohexylphosphino)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 gel plug which was washed with 10% solution of methanol in ethyl acetate (75 mL) and the eluate was concentrated in vacuum. The residue was purified by preparative HPLC to give the title compound as a solid, 35 mg (58%).

情報源と証拠