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HRID 317作成日:2026年10月23日

Piperazine → 4-Chloro-2-(piperazin-1-yl)benzonitrile

https://huagongshe.com/ja/reaction/317

反応式

関与物質

役割名称HCID仕込み量
反応物PiperazineHCID 4837—
反応物2-Bromo-4-chlorobenzonitrileHCID 23498524—
試薬Cesium carbonateHCID 10796—
触媒Binap, (A+-)-HCID 634876—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒1,4-DioxaneHCID 31275—
生成物4-Chloro-2-(piperazin-1-yl)benzonitrileHCID 179292380%

反応条件

温度90 °C

反応手順

Tris(dibenzylideneacetone)dipalladium (0) (43.4 mg, 0.05 mmol) and rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (59.0 mg, 0.09 mmol) were added to a mixture of 2-bromo-4-chlorobenzonitrile (205 mg, 0.95 mmol), Cesium carbonate (463 mg, 1.42 mmol) and Piperazine (163 mg, 1.89 mmol) in dioxane (3 mL). Reaction vessel was placed in an oil bath set to 90 °C 2.45pm. LCMS o/n shows large product peak (222). Cooled, filtered through a silica plug, washing with EtOAc until filtrate is clear. Crude NMR is very messy, target deprioritized. Discarded.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-124e8e40d3e54042af531dbb1d8d85d1
出典メモ750 AstraZeneca ELN dataset