反应详情

Dissolve 4-{4-(3-chloro-4-fluoro-phenyl)-1-[2-(tetrahydro-pyran-2-yloxy)-ethyl]-1H-imidazol-2-yl}-piperidine-1-carboxylic acid tert-butyl ester (6.85 g; 13.48 mmol) in THF (200 mL) and add 1M aqueous hydrogen chloride (20 mL) and stir 18 h at RT. Dilute with EA, wash with saturated sodium bicarbonate, brine, dry with anhydrous MgSO4, filter, and evaporate. Purify the residue on 330 g silica gel with 2:1 DCM/EA to provide the title compound (5.07 g; 89%) as a white crystalline solid. MS (ES): m/z=424 (M+H).

1. washwash with saturated sodium bicarbonate, brine
2. dry with materialdry with anhydrous MgSO4
3. filtrationfilter
4. customevaporate
5. customPurify the residue on 330 g silica gel with 2:1 DCM/EA