[N:1]1[CH:6]=[CH:5][C:4]([C:7]([F:14])([F:13])[C:8](OCC)=[O:9])=[CH:3][CH:2]=1.[BH4-].[Na+]>C(O)C>[F:14][C:7]([F:13])([C:4]1[CH:5]=[CH:6][N:1]=[CH:2][CH:3]=1)[CH2:8][OH:9]To a solution of ethyl pyridin-4-yl-difluoroacetate (0.59 g) prepared in (1) in ethanol (10 mL) was added NaBH4 (0.11 g) at 0° C. The reaction mixture was stirred at RT for 2 hr. The solvent was removed under reduced pressure. Water was added to the residue and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous NaHCO3, and then dried over MgSO4. The solvent was removed under reduced pressure. The residue was purified by silica gel chromatography (Developing solvent: ethyl acetate) to give the title compound (0.082 g, 1%).
Wird geladen…