反应详情

To a solution of 4-(2-bromo-5-fluorophenoxy)piperidine (2.0 g, 7.30 mmol) in THF (24.3 ml) was added cyanogen bromide (0.77 g, 7.30 mmol) followed by triethylamine (1.01 ml, 7.3 mmol) at 0° C. The mixture was warmed to rt and further stirred for 1 h. Solvent was evaporated and the residue was diluted with 1N HCl (20 mL). The aqueous layer was extracted with EtOAc (3×10 mL). The combined organic fractions were washed with water (20 mL) and dried over Na2SO4. The solvent was evaporated under reduced pressure to afford the title compound as a solid which was used in the next step without further purification.

1. customSolvent was evaporated
2. additionthe residue was diluted with 1N HCl (20 mL)
3. extractionThe aqueous layer was extracted with EtOAc (3×10 mL)
4. washThe combined organic fractions were washed with water (20 mL)
5. dry with materialdried over Na2SO4
6. customThe solvent was evaporated under reduced pressure