反应详情

PS-DCC (1.02 g, 1.35 mmol, loading: 1.33 mmol/g) was suspended in dry THF (13.5 ml). HOBT (0.21 g, 1.35 mmol), 2-((4-fluorophenyl)(methyl)amino)-2-phenylacetic acid hydrochloride (I6) (0.20 g, 0.68 mmol), and (R)-quinuclidin-3-ol (0.26 g, 2.03 mmol) were added. The mixture was shaken at RT overnight. PS-DCC was removed by filtration, washed with EtOAc and THF. The solution was evaporated, and the residue was partitioned between EtOAc and water. The organic phase was washed with saturated NaHCO3, dried with Na2SO4, and evaporated. The crude was purified by flash chromatography (DCM/MeOH=95/5) to afford the title compound (209 mg, 84% yield, mixture of diastereomers).

1. customPS-DCC was removed by filtration
2. washwashed with EtOAc and THF
3. customThe solution was evaporated
4. customthe residue was partitioned between EtOAc and water
5. washThe organic phase was washed with saturated NaHCO3
6. dry with materialdried with Na2SO4
7. customevaporated
8. customThe crude was purified by flash chromatography (DCM/MeOH=95/5)