Piperazine, 2-pyridylethyl- → Ethyl 7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxylate

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07/01 2009 12:44:11 +0100 To ethyl 7-bromobenzofuran-2-carboxylate (0.100 g, 0.37 mmol) and 1-(2-(pyridin-2-yl)ethyl)piperazine (0.075 g, 0.39 mmol) in dry degassed dioxane (1.5 mL) were added Cesium carbonate (0.157 g, 0.48 mmol), 2-Dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (0.018 g, 0.04 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (0.017 g, 0.02 mmol) under argon and the reaction heated at 95°C o/n. All starting material consumed. Water and DCM were added and the layers separated. The aq phase was extracted with DCM (3x). The combined org phases were washed with water, dried (MgSO4), filtered and evaporated. The crude was purified by flash (SiO2; DCM/MeOH 95/5) to give 0.0661 g of the product as a pale yellow semisolid.

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