反应详情

Stir a mixture of dichloroethane (25 mL), N-aminomorpholine (0.204 g, 2 mmol), (R)-4-((R)-4-benzyl-2-oxo-oxazolidin-3-yl)-3-(4-benzyloxy-2,6-dichloro-benzyl)-4-oxo-butyraldehyde (1.064 g, 2 mmol) and sodium triacetoxyborohydride (1.266 g, 6 mmol) at room temperature for 12 hours. Bring the reaction to 60° C. and stir for 3 hours. Cool the reaction, dilute with dichloromethane, and wash with water. Dry the organic layer (Na2SO4), remove the solvent in vacuo to afford crude product, and purify on silica with a 50 to 75% ethyl acetate in hexanes gradient to afford 0.07 g (80%) of the titled product. MS (m/z): 435 (M+).

1. customBring the reaction to 60° C.
2. stirringstir for 3 hours
3. temperatureCool
4. customthe reaction
5. washwash with water
6. dry with materialDry the organic layer (Na2SO4)
7. customremove the solvent in vacuo
8. customto afford crude product
9. custompurify on silica with a 50 to 75% ethyl acetate in hexanes gradient