反应详情

温度

80 °C

Cyclopropylmethyl bromide (0.072 ml, 0.75 mmol) was added to a suspension (5.0 ml) of 5-hydroxy-1-(toluene-4-sulfonyl)-1H-indole-2-carboxylic acid ethyl ester (173 mg, 0.48 mmol) and potassium carbonate (276 mg, 1.0 mmol) in acetonitrile, and stirred at 80° C. for five hours. After cooling to room temperature, the reaction mixture was combined with ethyl acetate and water and extracted with ethyl acetate. The extract was washed with water and a saturated aqueous solution of sodium chloride, and dried over anhydrous sodium sulfate. The desiccant was removed by filtration. The filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography to give 5-cyclopropylmethoxy-1-(toluene-4-sulfonyl)-1H-indole-2-carboxylic acid ethyl ester as a colorless gum-like material (112.5 mg, 56%).

1. temperatureAfter cooling to room temperature
2. extractionextracted with ethyl acetate
3. washThe extract was washed with water
4. dry with materiala saturated aqueous solution of sodium chloride, and dried over anhydrous sodium sulfate
5. customThe desiccant was removed by filtration
6. concentrationThe filtrate was concentrated under reduced pressure
7. customThe resulting residue was purified by silica gel column chromatography