反应详情

温度

100 °C

4-Bromo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine (1.546 g, 4.59 mmol), 1-(phenylsulfonyl)-6-(trimethylstannanyl)-1H-indazol-4-amine (2 g, 4.59 mmol) and Pd(Ph3P)4 (0.265 g, 0.229 mmol) were added to N,N-dimethylformamide (30 mL) under nitrogen. The mixture was heated at 100° C. for 2 days then cooled at room temperature 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 Companion and eluting with a gradient of 30 to 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 at room temperature
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 to 85% MeCN (+0.1% TFA)/H2O (0.1% TFA)
6. additionFractions containing desired product
7. customthe solvent was removed