反应详情

Combine (R)-4-[(1R,2S)-3-(3,5-difluorophenyl)-1-hydroxy-2-nitropropyl]-2,2-dimethyloxazolidine-3-carboxylic acid tert-butyl ester (1.13 g, 2.71 mmol) and nickel (II) chloride (0.58 g, 4.485 mmol) in dry methanol (30 ml) and add sodium borohydride (0.454 g, 12 mmol) over 1 minute. Stir the resulting mixture for 20 minutes and then add water (3 mL). Concentrate and dissolve the residue in ethyl acetate. Filter the black solution through a pad of Celite® and wash the filter cake with ethyl acetate. Wash the filtrate with water (twice), saturated aqueous sodium chloride, dry (magnesium sulfate), filter, and concentrate to give the desired compound as a white solid (920 mg, 95%).

1. concentrationConcentrate
2. dissolutiondissolve the residue in ethyl acetate
3. filtrationFilter the black solution through a pad of Celite®
4. washwash the filter cake with ethyl acetate
5. washWash the filtrate with water (twice), saturated aqueous sodium chloride
6. dry with materialdry (magnesium sulfate)
7. filtrationfilter
8. concentrationconcentrate