関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Piperazine, 2-pyridylethyl- | HCID 566605 | — |
| 反応物 | Ethyl 7-bromobenzofuran-2-carboxylate | HCID 46738833 | — |
| 試薬 | Cesium carbonate | HCID 10796 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 触媒 | 2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl | HCID 11155794 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | Ethyl 7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxylate | HCID 59636751 | 46.88% |
反応手順
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.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
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| ORD ID | ord-ca59850458054174b55daef8c9f3b978 |
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| 出典メモ | 750 AstraZeneca ELN dataset |
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