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HRID 459813作成日:2026年10月24日

Piperazine → 1-(3-Fluorophenyl)piperazine

https://huagongshe.com/ja/reaction/459813

反応式

関与物質

役割名称HCID仕込み量
反応物PiperazineHCID 4837—
反応物1-Bromo-3-fluorobenzeneHCID 14082—
反応物Binap, (A+-)-HCID 634876—
反応物Sodium t-butoxideHCID 23676156—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
溶媒Ethyl AcetateHCID 8857—
生成物1-(3-Fluorophenyl)piperazineHCID 77418—

反応手順

1 g (5.71 mmol) of 3-fluorobromobenzene and 2.95 g (34.29 mmol) of piperazine are dissolved in 20 ml of toluene, and 0.77 g (8 mmol) of sodium tert-butoxide is added. In the presence of 0.11 g (0.17 mmol) of BINAP and 0.05 g (0.06 mmol) of tris(dibenzylideneacetone)dipalladium, the mixture is then stirred under reflux overnight. After cooling, ethyl acetate is added and the mixture is washed with water. The mixture is then extracted with 1N hydrochloric acid, and the aqueous phase is washed with ethyl acetate. The pH is adjusted to 8–9 and the mixture is then extracted with dichloromethane. The organic phase is dried over magnesium sulphate and the solvent is removed, giving the target compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07196086B2
出典データセットuspto-grants-2007_03
ORD IDord-83ceb8398b0a4c5a9a0c9f3f58d2e4e7
出典メモuspto-grants-2007_03