反应详情

Ethanol (27.5 ml) was added to (2S, 3S)-3-tert-butoxycarbonylamino-1,2-epoxy-4-phenylbutane (2.75 g), followed by addition of aqueous 6.8% citric acid solution (29.5 g) and agitation at 70° C. for 2 hours. After cooling to ambient temperature, ethanol was removed under reduced pressure. The product was extracted by using ethyl acetate, followed by drying over anhydrous sodium sulfate and concentration under reduced pressure. Furthermore, a mixture solvent of hexane (2.5 ml) and ethyl acetate (2.5 ml) was added, to generate crystal. The crystal was filtered, and then, the crystal was rinsed twice by using a mixture solvent of hexane/ethyl acetate (1/1). The resulting crystal was dried, to afford the objective (4S, 5R)-5-hydroxymethyl-4-phenylmethyloxazolidin-2-one (1.79 g) in 80% yield.

1. customethanol was removed under reduced pressure
2. extractionThe product was extracted
3. dry with materialby drying over anhydrous sodium sulfate and concentration under reduced pressure
4. additionFurthermore, a mixture solvent of hexane (2.5 ml) and ethyl acetate (2.5 ml) was added
5. filtrationThe crystal was filtered
6. washthe crystal was rinsed twice
7. customThe resulting crystal was dried