Acetonitrile → HCID 178509577, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-chloro-6-{2-[4-(2-chlorophenyl)-1H-imidazol-2-yl]-4-morpholinyl}-2-pyrimidinamine (100 mg, 0.256 mmol), 2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile (82 mg, 0.332 mmol), Na2CO3 (67.7 mg, 0.639 mmol) and Pd(PPh3)4 (29.5 mg, 0.026 mmol) in 1,4-dioxane (4 mL) and water (1 mL) was heated at 140° C. under microwave conditions with stirring for 1 hour. The reaction mixture was filtered, washed by EtOAc (100 mL), and concentrated. The resulting residue was purified by prep-HPLC using CH3CN in water (10 mmol NH4HCO3 in water) from 60% to 70% in 7 minutes to afford the title compound (50 mg) as a yellow solid. LC-MS (ES) m/z=476 [M+H]+.

Provenance & Evidence