反应详情

To a solution of [2-(2-[1,3]dioxolan-2-yl-phenyl)-6-methoxy-benzo[b]thiophen-3-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone (crude) in THF (15 mL), add HCl (2 mL, 5M) and water (2 mL). Heat the mixture to reflux for 30 min. Dilute with CH2Cl2 and quench with aq. NaHCO3. Wash the organic phase with water and brine, dry over MgSO4, filter and concentrate. Purify the crude product by flash chromatography (0-10% (2M NH3 in MeOH)/CH2Cl2) to afford 2-{6-methoxy-3-[4(2-piperidin-1-yl-ethoxy)-benzoyl]-benzo[b]thiophen-2-yl}-benzaldehyde (410 mg) which is contaminated with unidentified byproducts and is used without further purification.

1. temperatureHeat the mixture
2. temperatureto reflux for 30 min
3. customquench with aq. NaHCO3
4. washWash the organic phase with water and brine
5. dry with materialdry over MgSO4
6. filtrationfilter
7. concentrationconcentrate
8. customPurify the crude product by flash chromatography (0-10% (2M NH3 in MeOH)/CH2Cl2)