反应详情

温度

100 °C

To a solution of N-(2-bromo-3,6-dimethylthieno[2,3-b]pyridin-4-yl)-3-chlorobenzenesulfonamide (Example 77) (100 mg, 0.232 mmol) in water (1 mL) and 1,4-dioxane (2 mL) was added [3-(methyloxy)phenyl]boronic acid (52.8 mg, 0.347 mmol), bis(triphenylphosphine)palladium(II) chloride (16.26 mg, 0.023 mmol), potassium carbonate (96 mg, 0.695 mmol) and the mixture heated to 100° C. for 15 min using a microwave reactor. The mixture was then filtered through celite, washing with ethyl acetate (30 mL) and DCM (20 mL). The organics were then combined, dried (phase separation cartridge) and concentrated. The residue was then purified by MDAP (basic conditions), to afford the title compound (36.8 mg). LCMS (A) m/z: 459 [M+1]+, Rt 1.32 min (acidic).

1. filtrationThe mixture was then filtered through celite
2. washwashing with ethyl acetate (30 mL) and DCM (20 mL)
3. customdried
4. custom(phase separation cartridge)
5. concentrationconcentrated
6. customThe residue was then purified by MDAP (basic conditions)