反应详情

温度

0 °C

Potassium tert-butoxide (26.6 mg, 0.24 mmol) was added to a solution of 5-chloro-3-(2,4-dimethoxyphenyl)-3-(4-pyridin-4-ylpiperazin-1-yl)-1,3-dihydroindol-2-one (0.10 g, 0.22 mmol) in dimethylformamide (4 mL) at 0° C., and the mixture was stirred at 0° C. for 1 hour. Then 8-quinolinesulfonyl chloride (53.9 mg, 0.24 mmol) was added to the reaction solution while cooling in ice, and the mixture was stirred at room temperature for 12 hours. Water was cautiously added to the mixture, which was extracted twice with ethyl acetate. The combined organic phase was washed with water and saturated brine, dried over sodium sulfate and concentrated under reduced pressure. Chromatographic purification of the residue on silica gel (mobile phase gradient 0-7% methanol in dichloromethane) afforded 57.0 mg of the title compound.

1. temperaturewhile cooling in ice
2. stirringthe mixture was stirred at room temperature for 12 hours
3. extractionwas extracted twice with ethyl acetate
4. washThe combined organic phase was washed with water and saturated brine
5. dry with materialdried over sodium sulfate
6. concentrationconcentrated under reduced pressure
7. customChromatographic purification of the residue on silica gel (mobile phase gradient 0-7% methanol in dichloromethane)