反应详情

To a solution of Intermediate F (0.165 g, 0.32 mmol) in dichloroethane (10 mL) was added L-leucine cyclopentyl ester tosylate (0.197 g, 0.52 mmol) and sodium triacetoxyborohydride (0.151 g, 0.71 mmol). The mixture was stirred for 90 minutes, then quenched by addition of saturated ammonium chloride (20 mL). The product was extracted with dichloromethane (3 times 100 mL) and the combined organic extracts were dried (MgSO4), concentrated and purified by flash column chromatography (SiO2, ethyl acetate) to yield the desired product (0.089 g, 53% yield). LC/MS: m/z 701.25 [M+H]+

1. customquenched by addition of saturated ammonium chloride (20 mL)
2. extractionThe product was extracted with dichloromethane (3 times 100 mL)
3. dry with materialthe combined organic extracts were dried (MgSO4)
4. concentrationconcentrated
5. custompurified by flash column chromatography (SiO2, ethyl acetate)