反应详情

温度

110 °C

4-Bromo-1-(phenylsulfonyl)-1H-indole (8.52 g, 25.3 mmol, Intermediate 44) was dissolved in dry toluene (20 mL) under an N2(g) atmosphere before vinylstannane (16.07 g, 50.7 mmol) and bis[triphenylphosphine)palladium(II) acetate (0.95 g, 1.3 mmol) was added. The reaction was heated to 110° C. for 16 h cooled the reaction mixture to RT and filtered the reaction mixture through a celite pad, and evaporated the solvent. Dissolved the obtained oil in acetonitrile and hexanes, separated the phases. Evaporated the acetonitrile phase and purified the obtained crude product by flash chromatography using 30% DCM in hexanes. Isolated 4.4 g of the desired product as a white solid, yield 62%. MS (ESI+) for C16H13NO2S m/z 284 (M+H)+.

1. additionwas added
2. temperaturecooled the reaction mixture to RT
3. filtrationfiltered the reaction mixture through a celite pad
4. customevaporated the solvent
5. dissolutionDissolved the obtained oil in acetonitrile
6. customhexanes, separated the phases
7. customEvaporated the acetonitrile phase
8. custompurified the
9. customobtained crude product by flash chromatography