反应详情

温度

100 °C

6-Bromo-1-methyl-1H-indazol-4-amine (300 mg), {1-[(4-methylphenyl)sulfonyl]-1H-pyrrolo[2,3-b]pyridin-4-yl}boronic acid (482 mg), tripotassium phosphate (845 mg) and Pd(dppf)Cl2 (97 mg) were added to 1,4-dioxane (7 ml) and water (3.5 ml). The reaction mixture was heated in the microwave at 100° C. for 15 min. After this time the reaction mixture was partitioned between water (20 ml) and DCM (20 ml). The organic layer was extracted then put through hydrophobic frits. The solvent was removed to afford a crude mixture. The residue was purified by column chromatography on silica (100 g) eluting with a gradient of 0-100% ethyl acetate:cyclohexane. Fractions containing desired product were combined and concentrated in vacuo to afford the title compound, 312 mg as an orange solid.

1. customAfter this time the reaction mixture was partitioned between water (20 ml) and DCM (20 ml)
2. extractionThe organic layer was extracted
3. customThe solvent was removed
4. customto afford a crude mixture
5. customThe residue was purified by column chromatography on silica (100 g)
6. washeluting with a gradient of 0-100% ethyl acetate
7. additionFractions containing desired product
8. concentrationconcentrated in vacuo