反应详情

To a solution of 6-benzyl-2-(4-(2,4-difluorophenoxyl)piperidin-1-yl)-3-(isopropylamino)pyrido[3,4-b]pyrazin-6-ium bromide (7.2 g, 12.62 mmol) in DCM (126 ml) was added NaBH(OAc)3 (16.05 g, 76 mmol). The resulting solution was stirred at room temperature for 3 days. After DCM was removed under vacuum, EtOAc (200 mL) was added to re-dissolve the residue. Then saturated NaHCO3 (150 mL) was added and the mixture was vigorously stirred for 30 min. The organic layer was washed with water (50 mL) and brine (50 mL), and dried with anhydrous Na2SO4 overnight. Removal of the solvent gave the title compound (6.43 g) as a yellow solid, which was used without further purification. ESI-MS m/z [M+H]+ 494.10.

1. customAfter DCM was removed under vacuum, EtOAc (200 mL)
2. additionwas added
3. dissolutionto re-dissolve the residue
4. additionThen saturated NaHCO3 (150 mL) was added
5. stirringthe mixture was vigorously stirred for 30 min
6. washThe organic layer was washed with water (50 mL) and brine (50 mL)
7. dry with materialdried with anhydrous Na2SO4 overnight
8. customRemoval of the solvent