反应详情

温度

105 °C

A mixture of tert-butyl N-[(3S)-1-[3-chloro-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-3-piperidyl]carbamate (0.2225 mmol; 115.9 mg), potassium cyclopropyl trifluoroborate (0.3337 mmol; 50.90 mg), butyldi-1-adamantylphosphine (0.06674 mmol; 25.19 mg), cesium carbonate (0.6674 mmol; 217.4 mg) and palladium(II) acetate (0.04449 mmol; 9.994 mg) in water (0.5 mL) and Toluene (4.5 mL) was purged with Argon for 1 minute. The reaction mixture in a pressure tube was stirred at 105° C. for 3 days. The layers were separated. The organic later was concentrated. The residue was purified on silica eluted with 0 to 5% MeOH in DCM to afford tert-butyl N-[(3S)-1-[3-cyclopropyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-3-piperidyl]carbamate (129 mg, ˜100%).

1. customwas purged with Argon for 1 minute
2. customThe layers were separated
3. concentrationThe organic later was concentrated
4. customThe residue was purified on silica
5. washeluted with 0 to 5% MeOH in DCM