反应详情

Stir a mixture of (R)-3-(4-benzyloxy-2,6-dichloro-benzyl)-1-(4-hydroxy-piperidin-1-yl)-pyrrolidin-2-one (1.23 g, 2.75 mmol) and 15 mL of dichloromethane in an ice bath. Add pyridine (0.52 g, 6.6 mmol) followed by triisopropylsilyltrifluoromethane sulfonate (0.924 g, 3.02 mmol). Remove the cold bath and stir the reaction 12 hours at room temperature. Dilute the reaction with dichloromethane and wash with water. Dry the organic phase over sodium sulfate, filter, and concentrate. Purify the residue by silica gel chromatography by eluting with 4:1 hexanes:ethyl acetate to give 1.2 g (72%) of the title compound. MS (m/z): 605 (M+).

1. customRemove the cold bath
2. stirringstir
3. customthe reaction 12 hours at room temperature
4. additionDilute
5. washwash with water
6. dry with materialDry the organic phase over sodium sulfate
7. filtrationfilter
8. concentrationconcentrate
9. customPurify the residue by silica gel chromatography
10. washby eluting with 4:1 hexanes