反应详情

温度

120 °C

Under Ar(g) to a mixture of compound 5 (20 mg, 0.069 mmol), 7-azaindole-4-boronic acid pinacol ester (18.5 mg, 0.076 mmol), dichloro-bis(triphenylphosphine)palladium (II) (2.4 mg, 0.003 mmol) and sodium hydrogen carbonate (17.4 mg, 0.21 mmol) was added ethanol (1 mL) followed by toluene (1.6 mL) and then water (0.5 mL). The reaction mixture was then heated in a microwave at 120° C. (300 W) for 1 h, and was subsequently cooled to rt; the mixture was then partitioned between CH2Cl2 and water, and the organic layer was separated, dried (MgSO4) and concentrated in vacuo. Purification by flash column chromatography on silica (eluant 30-90% EtOAc/Hex) furnished D (20 mg, 0.054 mol, 78%) as an off-white solid.

1. temperaturewas subsequently cooled to rt
2. customthe mixture was then partitioned between CH2Cl2 and water
3. customthe organic layer was separated
4. dry with materialdried (MgSO4)
5. concentrationconcentrated in vacuo
6. customPurification by flash column chromatography on silica (eluant 30-90% EtOAc/Hex)
7. customfurnished D (20 mg, 0.054 mol, 78%) as an off-white solid