Potassium Carbonate → 2-[2-[1-(2-Methyl-pyrimidin-4-yl)-piperidin-4-ylamino]-6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yl]-propan-2-ol

Participants

Reaction Conditions

Reaction Steps

A mixture of palladium (II) acetate (2.7 mg, 0.012 mmol) and 2-(dicyclohexylphosphino)-biphenyl (8.4 mg, 0.024 mmol) in dioxane (1 mL) was stirred under argon at 20° C. for 10 minutes. The resulting catalyst solution was added to a suspension of potassium carbonate (692 mg, 5.0 mmol), 1-(2-methyl-pyrimidin-4-yl)-piperidin-4-ylamine dihydrochloride (80 mg, 0.3 mmol), and 2-[2-chloro-6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yl]-propan-2-ol (95 mg, 0.3 mmol) in dioxane (1.7 mL). The reaction mixture was heated to 170° C. in a microwave oven for 30 minutes. The reaction mixture was cooled, diluted with water and extracted twice with ethyl acetate. The organic layer was washed with brine, dried over sodium sulfate, and concentrated under reduced pressure. The crude product was purified by column chromatography on silica gel using CH2Cl2/0-10% MeOH as eluent. The title compound was obtained as a light yellow solid (9 mg, 6%).

Provenance & Evidence