反应详情

Place cis-1-[4-(tert-Butyl-dimethyl-silanyloxy)-cyclohexyl]-piperidin-2-one, (300 mg, 0.96 mmol) in 7.0 mL of THF, cool to −78° C. and treat with 2.0 M LDA (0.72 mL, 1.5 mmol). Stir for 5.0 minutes, treat with 2-bromomethyl-3-chloro-benzo[b]thiophene (250 mg, 0.96 mmol) and stir at −78° C. for five hours, and warm to room temperature. Quench reaction with ammonium chloride, extract with dichloromethane, dry over sodium sulfate and purify via silica chromatography (ethyl acetate/hexanes 0-25%) affords 166 mg (35%).

1. stirringstir at −78° C. for five hours
2. customQuench
3. customreaction with ammonium chloride
4. extractionextract with dichloromethane
5. dry with materialdry over sodium sulfate
6. custompurify via silica chromatography (ethyl acetate/hexanes 0-25%)
7. customaffords 166 mg (35%)