反应详情

Ethyl 4-(S)-benzyloxycarbonylamino-4-cyclopropyl-3-oxobutanoate (1.526 g, 4.778 mmol) was dissolved in anhydrous ethanol (15 ml), and the solution was mixed with sodium borohydride (94.6 mg, 2.50 mmol)under ice-cooling and stirred at the same temperature for 1 hour. Under ice-cooling, the reaction solution was mixed with water (20 ml) and then ethanol was evaporated under a reduced pressure. The thus obtained residue was mixed with chloroform (50 ml) and stirred, and then the thus separated chloroform layer was washed with saturated sodium chloride aqueous solution (30 ml) and dried over anhydrous magnesium sulfate. After filtration, the solvent was evaporated to dryness under a reduced pressure, thereby obtaining 1.509 g (98.3%) of the title compound as a colorless oil. This product was used in the subsequent reaction without purification.

1. temperaturecooling
2. temperatureUnder ice-cooling
3. customethanol was evaporated under a reduced pressure
4. additionThe thus obtained residue was mixed with chloroform (50 ml)
5. stirringstirred
6. washthe thus separated chloroform layer was washed with saturated sodium chloride aqueous solution (30 ml)
7. dry with materialdried over anhydrous magnesium sulfate
8. filtrationAfter filtration
9. customthe solvent was evaporated to dryness under a reduced pressure