反应详情

温度

70 °C

1-(6-chloro-3-methoxy-1-trityl-1H-pyrazolo[4,3-c]pyridin-4-yl)prop-2-yn-1-one (60B, 63 mg, 0.132 mmol) was dissolved in acetonitrile (3 ml), charged with acetamidine hydrochloride (14.95 mg, 0.158 mmol) and sodium carbonate (34.9 mg, 0.330 mmol) and allowed to stir at 70° C. for 2 h. The solution was filtered through a syringe filter and the solvents were removed in vacuo. The residue was purified on silica gel 2-25% EtOAc/DCM to afford 6-chloro-3-methoxy-4-(2-methylpyrimidin-4-yl)-1-trityl-1H-pyrazolo[4,3-c]pyridine (63B, 58 mg, 0.112 mmol, 85% yield). MS: [M+H]+ m/z 518.

1. filtrationThe solution was filtered through a syringe
2. filtrationfilter
3. customthe solvents were removed in vacuo
4. customThe residue was purified on silica gel 2-25% EtOAc/DCM