反应详情

Add acetic anhydride (0.07 g, 0.70 mmol) to (2R,3S,5R)-5-[2-Amino-3-(3-fluoro-5-propoxy-phenyl)-1-hydroxy-propyl]-2-(2,2-dimethyl-propoxy)-3-methyl-morpholine-4-carboxylic acid tert-butyl ester (0.34 g, 0.66 mmol) and triethylamine (0.10 g, 0.99 mmol) in tetrahydrofuran (6 mL) at room temperature and stir 1 hour. Dilute with ethyl acetate and wash with saturated aqueous ammonium chloride and saturated aqueous sodium chloride. Dry over magnesium sulfate, filter and concentrate. Purify on 12 g silica gel eluting with 100:0 to 20:80 hexanes:ethyl acetate to give 0.175 g of the desired compound as an oil.

1. washwash with saturated aqueous ammonium chloride and saturated aqueous sodium chloride
2. dry with materialDry over magnesium sulfate
3. filtrationfilter
4. concentrationconcentrate
5. customPurify on 12 g silica gel eluting with 100:0 to 20:80 hexanes