反应详情

温度

50 °C

A mixture of 7-[2-methoxy-1-(methoxymethyl)ethoxy]-5-{[6-(methylsulfonyl)pyridin-3-yl]oxy}-1H-indole-2-carboxylic acid (1.02 g), N-ethyl-N′-(3-dimethylaminopropyl)carbodiimide hydrochloride (868 mg), 1-hydroxybenzotriazole (612 mg) and N,N-dimethylformamide (20 mL) was stirred at 50° C. for 25 min. The mixture was cooled to room temperature, and 10% ammonium hydroxide solution (3 mL) was added to the mixture. After stirring at room temperature for 2 days, the mixture was concentrated under reduced pressure. Water was added to the residue and the mixture was extracted with ethyl acetate. The organic layer was washed successively with water and saturated brine, dried over magnesium sulfate, filtered and concentrated to give the title compound (1.08 g, 100%) as an orange oil. MS 450 (MH+).

1. temperatureThe mixture was cooled to room temperature
2. stirringAfter stirring at room temperature for 2 days
3. concentrationthe mixture was concentrated under reduced pressure
4. additionWater was added to the residue
5. extractionthe mixture was extracted with ethyl acetate
6. washThe organic layer was washed successively with water and saturated brine
7. dry with materialdried over magnesium sulfate
8. filtrationfiltered
9. concentrationconcentrated