反应详情

温度

110 °C

A mixture of 6-[1-(6-fluoro-2-pyridyl)pyrazolo[4,3-c]pyridin-6-yl]-N-[(4-methoxyphenyl)methyl]pyrazin-2-amine (0.479 mmol; 316.3 mg), tert-butyl 1,4-diazepane-1-carboxylate (0.958 mmol; 192 mg), and N-Methylmorpholine (1.20 mmol; 122 mg; 0.133 mL) in 1-methyl-2-pyrrolidinone (5 mL) in a sealed pressure vial was heated at 110° C. overnight. The mixture was poured into water, and extracted with EtOAc. The organic layer was concentrated. The residue was purified on silica eluted with 0 to 100% EtOAc in DCM to afford tert-butyl 4-[6-[6-[6-[(4-methoxyphenyl)methylamino]pyrazin-2-yl]pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-1,4-diazepane-1-carboxylate (˜291 mg, 100%).

1. extractionextracted with EtOAc
2. concentrationThe organic layer was concentrated
3. customThe residue was purified on silica
4. washeluted with 0 to 100% EtOAc in DCM