反应详情

To a solution of 232a (1.2 g, 5.8 mmol) in CH3OH (25 mL) was added HCHO (1 mL, 35 mmol) and acetic acid (1 mL), followed by the addition of NaBHCN3 (1.0 g, 12 mmol). The mixture was stirred at room temperature for 2 h. It was then evaporated under reduced pressure and the residue was purified by reverse-phase Combiflush eluting with 0.3% NH4HCO3 in water/acetonitrile to afford 232b as a yellow solid (1.0 g, 78%). MS-ESI: [M+H]+ 220.

1. additionfollowed by the addition of NaBHCN3 (1.0 g, 12 mmol)
2. customIt was then evaporated under reduced pressure
3. customthe residue was purified by reverse-phase Combiflush
4. washeluting with 0.3% NH4HCO3 in water/acetonitrile