反应详情

温度

150 °C

A mixture of [(3S)-1-[6-(6-chloropyrazolo[4,3-c]pyridin-1-yl)-3-cyano-2-pyridyl]-3-piperidyl]carbamic acid (0.5166 mmol; 205.5 mg), trimethyl-(6-methylpyrazin-2-yl)stannane (0.7749 mmol; 199.1 mg), and palladium(0)tetrakis (triphenylphosphine); (0.05166 mmol; 59.8 mg) in N,N-Dimethylacetamide (12 mL) was purged with Argon. The reaction mixture was sealed in a pressure vial and heated at 150° C. for 2 hours. The mixture was cooled to room temperature, and then partitioned between EtOAc and water. The organic layer was concentrated and the residue was purified on silica eluted with 0 to 5% MeOH in DCM to afford tert-butyl N-[(3S)-1-[3-cyano-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-3-piperidyl]carbamate as a yellow solid (248.6 mg, 94%).

1. custom(0.05166 mmol; 59.8 mg) in N,N-Dimethylacetamide (12 mL) was purged with Argon
2. customThe reaction mixture was sealed in a pressure vial
3. temperatureThe mixture was cooled to room temperature
4. custompartitioned between EtOAc and water
5. concentrationThe organic layer was concentrated
6. customthe residue was purified on silica
7. washeluted with 0 to 5% MeOH in DCM