反应详情

温度

80 °C

To a solution of 6-bromo-4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3,4-oxadiazol-2-yl)-1-(phenylsulfonyl)-1H-indazole (0.82 g, 1.540 mmol) in 1,4-dioxane (15 ml) and water (1.5 ml) was added 2-(methyloxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3-pyridinamine (0.501 g, 2.002 mmol), 1,1′-bis(diphenylphosphino)ferrocene palladium dichloride (0.225 g, 0.308 mmol) and potassium phosphate tribasic (0.981 g, 4.62 mmol). The mixture was heated at 80° C. for 2 hr, cooled and concentrated in vacuo and the residue partitioned between dichloromethane and water (20 ml), separated by hydrophobic frit and purified by silica (100 g) cartridge on Flashmaster II, using a gradient of dichloromethane and methanol (1% triethylamine) to give the title compound as an orange solid (0.88 g).

1. temperaturecooled
2. concentrationconcentrated in vacuo
3. customthe residue partitioned between dichloromethane and water (20 ml)
4. customseparated by hydrophobic frit
5. custompurified by silica (100 g) cartridge on Flashmaster II