反应详情

温度

30 °C

Stir tert-butyl 4-(6-hydroxypyridin-2-yl)piperidine-1-carboxylate (0.25 g, 0.90 mmol) in DMF (10 mL) and add cesium carbonate (0.44 g, 1.35 mmol) and (bromomethyl)cyclopropane (0.13 g, 0.99 mmol). Heat the mixture to 30° C. and stir overnight. Quench the reaction with water, and extract three times with EtOAc (20 mL). Combine the organic extracts. Wash the extracts with water then brine; dry over sodium sulphate; collect the filtrate; and concentrate under vacuum to give the crude product. Purify using silica gel normal phase flash column chromatography using a gradient of 0-30% ethyl acetate in petroleum ether to give the title compound (0.28 g, 94%) as a clear oil. MS (m/z): 333 (M+1).

1. customQuench
2. customthe reaction with water
3. extractionextract three times with EtOAc (20 mL)
4. washWash the extracts with water
5. dry with materialdry over sodium sulphate
6. customcollect the filtrate
7. concentrationand concentrate under vacuum
8. customto give the crude product
9. customPurify