反应详情

(1S,5S)-7-Hydroxy-4-oxo-3-[(1R)-1-phenylethyl]-3-azabicyclo[3.3.0]octan-1-ylcarboxylic acid tert-butyl ester (1.0 g, 2.89 mmol) was dissolved in methylene chloride (15 mL). Bis(2-methoxyethyl)aminosulfur trifluoride (BAST) (0.59 mL) was added under ice-cooling, and the mixture was stirred at the same temperature for one hour. The reaction solution was washed with saturated sodium bicarbonate water, dried over magnesium sulfate, and filtered. Then, the solvent was evaporated under reduced pressure. The residue was purified by silica gel chromatography (hexane:ethyl acetate=10:1→4:1→1:1) to give 711 mg (71%) of the title compound as a colorless oil.

1. temperaturecooling
2. washThe reaction solution was washed with saturated sodium bicarbonate water
3. dry with materialdried over magnesium sulfate
4. filtrationfiltered
5. customThen, the solvent was evaporated under reduced pressure
6. customThe residue was purified by silica gel chromatography (hexane:ethyl acetate=10:1→4:1→1:1)