Potassium Carbonate → N-(2,4-difluoro-3-[5-(1H-indazol-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-2,5-difluoro-benzenesulfonamide

Participants

Reaction Conditions

Reaction Steps

Into a microwave vial, 5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-indazole (12, 28 mg, 0.11 mmol) is combined with N-[3-(5-bromo-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide (26, 50 mg, 0.09 mmol), tetrakis(triphenylphosphine)palladium(0) (2.2 mg, 0.0019 mmol), and potassium carbonate (1.0 mL, 1.0 M in water) in 3 mL of acetonitrile. The reaction is heated at 140° C. for 50 minutes in a microwave, the solvents removed under vacuum, and the residue purified by silica gel column chromatography, eluting with dichloromethane and methanol. Appropriate fractions are combined and concentrated under vacuum to provide the desired compound as a white solid (P-0002, 28 mg, 50%). MS (ESI) [M+H+]+=565.85.

Provenance & Evidence