反应详情

To a stirred solution of (1S)-{4-[(5-tert-butoxycarbonylamino-1-hydroxymethyl-pentyl)-isobutyl-sulfamoyl]-phenyl}-carbamic acid tert-butyl ester (intermediate product (VII) of example 1, step D, 97 mg, 0.18 mmol) in anhydrous CH2Cl2 (3 mL) was added N,N-dimethylaminopyridine (22 mg, 0.18 mmol) and acetic anhydride (0.014 mL, 0.18 mmol). The mixture was stirred at room temperature for 1 hour. The solvent was evaporated. Ethyl acetate (50 mL) was added and the organic layer was washed with water (30 mL), then dried with Na2SO4 and concentrated. The residue was purified by flash chromatography eluting with ethyl acetate. The yield obtained was quantitative (100 mg).

1. customThe solvent was evaporated
2. additionEthyl acetate (50 mL) was added
3. washthe organic layer was washed with water (30 mL)
4. dry with materialdried with Na2SO4
5. concentrationconcentrated
6. customThe residue was purified by flash chromatography
7. washeluting with ethyl acetate
8. customThe yield obtained