反应详情

温度

100 °C

A mixture of 6-(6-methylpyrazin-2-yl)-1H-pyrazolo[4,3-c]pyridine (0.4734 mmol; 100.0 mg), tert-butyl N-[(3S)-1-(6-bromo-3-methoxy-2-pyridyl)-3-piperidyl]carbamate (0.5681 mmol, 219.5 mg), N,N′-Dimethylethylenediamine (0.4734 mmol; 41.73 mg; 0.0471 mL), copper iodide (0.4734 mmol; 91.08 mg), and potassium carbonate (0.5208 mmol; 72.70 mg) in 1,4-Dioxane (10 mL) was purged with Argon, then sealed and stirred at 100° C. overnight. The mixture was cooled to room temperature, and then filtered through Celite. The filtrate was concentrated; the residue was purified on silica eluted with 0 to 100% EtOAc in DCM to afford tert-butyl N-[(3S)-1-[3-methoxy-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-3-piperidyl]carbamate as a tan solid (142.5 mg, 58%).

1. customwas purged with Argon
2. customsealed
3. temperatureThe mixture was cooled to room temperature
4. filtrationfiltered through Celite
5. concentrationThe filtrate was concentrated
6. customthe residue was purified on silica
7. washeluted with 0 to 100% EtOAc in DCM