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HRID 535680作成日:2026年10月25日

Piperazine, 2-pyridylethyl- → 5-Methoxy-N,N-dimethyl-7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxamide

https://huagongshe.com/reaction/535680

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2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenylHCID 11155794—
反応物Sodium t-butoxideHCID 23676156—
反応物7-Bromo-5-methoxy-N,N-dimethylbenzofuran-2-carboxamideHCID 59636744—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
溶媒Ethyl AcetateHCID 8857—
生成物5-Methoxy-N,N-dimethyl-7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxamideHCID 59636711—

反応手順

7-Bromo-5-methoxy-N,N-dimethylbenzofuran-2-carboxamide (0.20 g, 0.67 mmol), 1-(2-pyridin-2-yl-ethyl)piperazine (0.13 g, 0.67 mmol), Pd2 dba3 (0.031 g, 0.030 mmol), 2-dicyclohexylphosphino-2′,4′,6′-tri-iso-propyl-1,1′-biphenyl (0.032 g, 0.070 mmol) and sodium t-butoxide (0.14 g, 1.41 mmol) were heated in toluene (1 mL) at 100° C. for 2 h. The mixture was allowed to cool. Ethyl acetate was added and the mixture was filtered through a pad of celite. The filtrate was washed with water and brine, dried over MgSO4 and the solvent was removed by rotary evaporation. The crude product was purified by flash chromatography (SiO2; DCM/MeOH; gradient 0-3%) to give the title compound. Yield: 0.14 g (52%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08859534B2
出典データセットuspto-grants-2014_10
ORD IDord-e8ee74b43f8e49dc9f0fc656bba9c955
出典メモuspto-grants-2014_10