反应详情

温度

100 °C

4-Bromo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine (1.546 g), 1-(phenylsulfonyl)-6-(trimethylstannanyl)-1H-indazol-4-amine (2 g) and Pd(PPh3)4 (0.265 g) were added to DMF (30 ml) under nitrogen. The mixture was heated at 100° C. for 2 days then cooled to RT and concentrated in vacuo. The mixture was purified by column chromatography on silica (70 g) eluting with ammonia and methanol in DCM, then again using the ISCO Companion, eluting with a gradient of 30-85% MeCN (+0.1% TFA): H2O (0.1% TFA). Fractions containing desired product were combined and the solvent was removed to afford the title compound as a brown solid (663 mg).

1. temperaturethen cooled to RT
2. concentrationconcentrated in vacuo
3. customThe mixture was purified by column chromatography on silica (70 g)
4. washeluting with ammonia and methanol in DCM
5. washeluting with a gradient of 30-85% MeCN (+0.1% TFA)
6. additionFractions containing desired product
7. customthe solvent was removed