反应详情

To a solution of 3-[5-(3-methyl-thiophen-2-yl)-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl]-propionaldehyde (Prep29, 16 mg, 0.04 mmol) in DCE (3 mL), (1S,5R)-1-(4-trifluoromethyl-phenyl)-3-aza-bicyclo[3.1.0]hexane (Prep4, 20 mg, 0.05 mmol) in DCE (1 mL), AcOH (6 μl, 0.05 mmol) and NaBH(AcO)3 (30 mg, 0.08 mmol) were added and the mixture was stirred at room temperature overnight. Diethylether was then added and the mixture was washed with 1N solution of HCl, then with aqueous saturated NaHCO3. The organic phase was dried (Na2SO4) and evaporated. The crude was purified by flash chromatography with DCM-MeOH—NH4OH (97-3-1) to give the title compound (8 mg, 42% yield) as a free base.

1. washthe mixture was washed with 1N solution of HCl
2. dry with materialThe organic phase was dried (Na2SO4)
3. customevaporated
4. customThe crude was purified by flash chromatography with DCM-MeOH—NH4OH (97-3-1)