反应详情

温度

95 °C

Cesium carbonate (0.724 g, 2.22 mmol), 2-dicyclohexylphosphino-2′,4′,6′-triisopropylbiphenyl (0.081 g, 0.17 mmol) and tris(dibenzylideneacetone)dipalladium(0) (0.078 g, 0.09 mmol) were added under argon to a mixture of ethyl 7-bromobenzofuran-2-carboxylate (0.460 g, 1.71 mmol) and 1-(5-(2-(piperazin-1-yl)ethyl)indolin-1-yl)ethanone (0.491 g, 1.79 mmol) (example 38c) in dry degassed dioxane (8 mL) and the reaction was heated at 95° C. over night. After cooling to room temperature, water and DCM were added and the layers separated. The aq phase was extracted with DCM (3×). The combined organic phases were washed with water, dried (MgSO4), filtered and evaporated. The crude product was purified by flash chromatography (DCM/MeOH 95/5) to give 0.485 g (61%) of the product.

1. customin dry
2. customdegassed dioxane (8 mL)
3. temperatureAfter cooling to room temperature
4. additionwater and DCM were added
5. customthe layers separated
6. extractionThe aq phase was extracted with DCM (3×)
7. washThe combined organic phases were washed with water
8. dry with materialdried (MgSO4)
9. filtrationfiltered
10. customevaporated
11. customThe crude product was purified by flash chromatography (DCM/MeOH 95/5)