反应详情

温度

140 °C

A mixture of 2,2-dimethyl-1-(2-tributylstannanyl-5H-pyrrolo[2,3-b]pyrazin-7-yl)-propan-1-one (115 mg, 0.23 mmol), 2-bromo-6-pyrrolidin-1-yl-pyridine (53 mg, 0.23 mmol), and Pd(PPh3)4 (27 mg, 0.023 mmol) in dioxane (1 mL) was stirred at 140° C. in a microwave for 1 h. The resulting mixture was treated with additional Pd(PPh3)4 (27 mg, 0.023 mmol), stirred at 150° C. in a microwave for 30 min, and concentrated. The crude product was purified by flash chromatography using 4 g of silica gel and EtOAc in hexanes as eluant, 3 consecutive purifications by preparative thin layer chromatography using 2:1 hexanes:EtOAc as eluant, and a recrystallization from CH2Cl2 and ethyl ether to provide 1.5 mg of 2,2-dimethyl-1-[2-(6-pyrrolidin-1-yl-pyridin-2-yl)-5H-pyrrolo[2,3-b]pyrazin-7-yl]-propan-1-one as a yellow powder. M+H 350.

1. stirringstirred at 150° C. in a microwave for 30 min
2. concentrationconcentrated
3. customThe crude product was purified by flash chromatography
4. customEtOAc as eluant, and a recrystallization from CH2Cl2 and ethyl ether