反应详情

Add borane-THF complex (10.69 mL, 10.7 mmol) to a solution of N-(1-(2-bromo-4-fluorophenyl)ethyl)-2,2-difluoroacetamide (1.06 g, 3.56 mmol) in THF (3 mL). Reflux the mixture for 17 h. Quench with hydrochloric acid (5 N, 8 mL). Stir the solution for 1 h. Add saturated NaHCO3. Dilute the mixture with DCM, wash with water and aqueous saturated sodium chloride. Separate the organic layer and dry over sodium sulfate. Filter and concentrate in vacuo to give the title compound (0.94 g, 93%). MS (ES) m/z 282 [M+1]+.

1. temperatureReflux the mixture for 17 h
2. customQuench with hydrochloric acid (5 N, 8 mL)
3. additionDilute the mixture with DCM
4. washwash with water and aqueous saturated sodium chloride
5. customSeparate the organic layer
6. dry with materialdry over sodium sulfate
7. filtrationFilter
8. concentrationconcentrate in vacuo