反应详情

To a mixture of (R)-3-(3,5-Dichloro-4′-methanesulfonyl-biphenyl-4-ylmethyl)-1-(4-triisopropylsilanyloxy-piperidin-1-yl)-pyrrolidin-2-one (0.12 g) in THF (6 mL), add water (6 mL) and TFA (2 mL). Stir the mixture at room temperature for 12 hours. Dilute the reaction mixture with ethyl acetate and wash with sodium bicarbonate (Sat.) and water. Separate the organic and dry over sodium sulfate, filter and concentrate. Purify the crude mixture on silica gel column with 50% ethyl acetate in hexane to 100% ethyl acetate to afford 0.088 g of the titled product. MS (m/z): 497 (M+).

1. washwash with sodium bicarbonate (Sat.) and water
2. customSeparate the organic and
3. dry with materialdry over sodium sulfate
4. filtrationfilter
5. concentrationconcentrate
6. customPurify the crude mixture on silica gel column with 50% ethyl acetate in hexane to 100% ethyl acetate