反应详情

Add triethylamine (0.030 g, 0.30 mmol) and acetic anhydride (0.024 g, 0.23 mmol) to R)-5-[(1S,2S)-2-amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2-ethoxymorpholine-4-carboxylic acid tert-butyl ester (0.095 g, 0.228 mmol) in tetrahydrofuran (4 mL) at room temperature. Stir 4 hours and dilute with ethyl acetate. Wash with water and saturated aqueous sodium chloride, dry (magnesium sulfate), concentrate and purify (silica gel chromatography, eluting with 20:80 to 100:0 ethyl acetate:hexanes) to give the desired compound (69 mg, 66%).

1. washWash with water and saturated aqueous sodium chloride
2. dry with materialdry (magnesium sulfate)
3. concentrationconcentrate
4. custompurify
5. wash(silica gel chromatography, eluting with 20:80 to 100:0 ethyl acetate:hexanes)