反应详情

To a solution of 2(5-fluoro-2-methyl-1H-indol-1-yl)acetic acid (1.29 g, 1.49 mmol), 2-(phenylsulfonyl)benzaldehyde (1.50 g, 6.10 mmol) and triethylsilane (4.30 ml, 27.0 mmol) in dichloromethane (40 ml) was added trifluoroacetic acid (1.25 ml, 16.5 mmol) dropwise under N2 at 0° C. over 30 minutes. The reaction was warmed to room temperature and stirred for 2 hours. Saturated aqueous sodium hydrogen carbonate solution was added and the product extracted with dichloromethane. The combined organic extracts were washed with saturated brine, dried over MgSO4 and concentrated in vacuo giving a brown oil which was triturated with petroleum ether (40-60° C.) to give a white solid (1.34 g, 2.88 mmol 52%).

1. extractionthe product extracted with dichloromethane
2. washThe combined organic extracts were washed with saturated brine
3. dry with materialdried over MgSO4
4. concentrationconcentrated in vacuo
5. customgiving a brown oil which
6. customwas triturated with petroleum ether (40-60° C.)
7. customto give a white solid (1.34 g, 2.88 mmol 52%)