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HRID 737131作成日:2026年10月27日

Toluene → 3-Benzyl-1-(5'-chloro-2'-methyl-biphenyl-4-ylmethyl)-piperazine

https://huagongshe.com/reaction/737131

反応式

関与物質

役割名称HCID仕込み量
反応物TolueneHCID 1140—
反応物Sodium CarbonateHCID 10340—
反応物(5-Chloro-2-methylphenyl)boronic acidHCID 2773336—
反応物3-(S)-benzyl-1-(4-bromobenzyl)-piperazineHCID 57849462—
触媒HCID 178418397HCID 178418397—
溶媒EthanolHCID 702—
生成物3-Benzyl-1-(5'-chloro-2'-methyl-biphenyl-4-ylmethyl)-piperazineHCID 7658273968%

反応条件

温度85 °C

反応手順

0.1 g of 3-(S)-benzyl-1-(4-bromo-benzyl)-piperazine were combined with 1.5 equiv. of 5-chloro-2-methylphenyl boronic acid, 0.05 equiv. of tetrakis(triphenylphosphine)palladium(0), 6 equiv. of 2M aqueous sodium carbonate solution, toluene and ethanol. The reaction mixture was heated at 85° C. under nitrogen overnight. The reaction mixture was concentrated in vacuo. The residue was diluted with water and extracted with ethyl acetate. The combined organic phases were washed with brine, dried over sodium sulfate, filtered and concentrated in vacuo. The crude material was purified by flash chromatography to afford 0.077 g of the title compound. Yield 68% ES MS (+) m/z 391.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07595397B2
出典データセットuspto-grants-2009_09
ORD IDord-840f17cf7ee241799f5b51c086c5d40d
出典メモuspto-grants-2009_09