反应详情

Suspend sodium hydride (0.45 g, 11.15 mmol) in 10 ml of dry dimethylformamide at 0° C. After stirring for 10 minutes, add the solution of (R)-3-(4-benzyloxy-2,6-dichloro-benzyl)-trans-1-(4-hydroxy-cyclohexyl)-pyrrolidin-2-one (2.50 g, 5.58 mmol) in 5 ml of dry dimethylformamide. Stir the resulting mixture for 15 minutes at 0° C. Add iodomethane (1.40 ml, 22.32 mmol) and allow the mixture to warm to room temperature. Stir the reaction at room temperature for an additional 12 hours then quench with water and filter the white precipitate. Dry under vacuum to recover 2.59 g of the title compound: MS (m/z): 462 (M+).

1. customat 0° C
2. stirringStir the resulting mixture for 15 minutes at 0° C
3. stirringStir
4. customthe reaction at room temperature for an additional 12 hours
5. customthen quench with water
6. filtrationfilter the white precipitate
7. customDry under vacuum
8. customto recover 2.59 g of the title compound