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HRID 100作成日:2026年10月24日

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

https://huagongshe.com/ja/reaction/100

反応式

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-carboxylateHCID 46738833—
試薬Cesium carbonateHCID 10796—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
触媒2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenylHCID 11155794—
溶媒1,4-DioxaneHCID 31275—
生成物Ethyl 7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxylateHCID 5963675146.88%

反応条件

温度95 °C

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
ORD IDord-ca59850458054174b55daef8c9f3b978
出典メモ750 AstraZeneca ELN dataset