反应详情

(R)-quinuclidin-3-yl 2-(tert-butoxycarbonylamino)-2-phenylacetate (C1) (5.17 g, 14.3 mmol) was dissolved in THF (47.8 ml) and, while stirring at RT, 37% HCl (4.71 ml, 57.4 mmol) was added dropwise. The reaction was stirred at RT for 15 hours overnight. The solvent was evaporated, and the residue was dissolved in DCM/MeOH (9/1; 10 ml) and about 3 g of SiO2 was added. The solvent was evaporated, and the solid was loaded on a silica gel column and eluted with DCM/MeOH/NH4OH (9/1/0.1) to obtain (R)-quinuclidin-3-yl 2-amino-2-phenylacetate (2.23 g; 60% yield).

1. stirringThe reaction was stirred at RT for 15 hours overnight
2. customThe solvent was evaporated
3. dissolutionthe residue was dissolved in DCM/MeOH (9/1; 10 ml)
4. additionabout 3 g of SiO2 was added
5. customThe solvent was evaporated
6. washeluted with DCM/MeOH/NH4OH (9/1/0.1)