反应详情

4-Bromomethyl-1-(tetrahydro-pyran-2-yl)-1H-indazole (0.5 g, 1.69 mmol), 3-(4′,5′-difluoro-2′-methoxy-biphenyl-4-ol (0.4 g, 1.69 mmol) and potassium carbonate (0.23 g, 1.69 mmol) in 15 mL THF/3 mL DMF was heated to 70° C. overnight. The reaction was cooled and distributed between EtOAc and H2O. The organic layer was separated and concentrated in vacuo. The crude product was purified by flash chromatography with a gradient from 0-25% ethyl acetate in hexanes to yield 4-(4′,5′-difluoro-2′-methoxy-biphenyl-4-yloxymethyl)-1-(tetrahydro-pyran-2-yl)-1H-indazole as a white solid (400 mg, 52.5%). HR-MS (ES) calculated for C26H24F2N2O3, 473.1646; found m/z 473.1647 [M+Na]+.

1. temperatureThe reaction was cooled
2. customThe organic layer was separated
3. concentrationconcentrated in vacuo
4. customThe crude product was purified by flash chromatography with a gradient from 0-25% ethyl acetate in hexanes