反应详情

To 5 ml of a methylene chloride solution of 149 mg of 2-[(1R,2S)-2-{(S)-2-cyclohexylmethoxycarbonylamino-4-methylvalerylamino}-1-hydroxy-3-methylbutyl]-3-phenylcyclopropenone obtained in Example 2 were added 81 mg of acetyl chloride and 102 mg of triethylamine. The resultant mixture was stirred at room temperature for 3 hours, mixed with diluted hydrochloric acid and shaken with methylene chloride. The organic layer was washed with water, saturated aqueous sodium bicarbonate and saturated brine in that order, dried over magnesium sulfate and filtered. The filtrate was concentrated and chromatographed on a column of silica gel, eluting with hexane:ethyl acetate (1:1) to give 73 mg of the titled product.

1. washThe organic layer was washed with water, saturated aqueous sodium bicarbonate and saturated brine in that order
2. dry with materialdried over magnesium sulfate
3. filtrationfiltered
4. concentrationThe filtrate was concentrated
5. customchromatographed on a column of silica gel
6. washeluting with hexane:ethyl acetate (1:1)