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HRID 383849作成日:2026年10月24日

Cesium carbonate → Ethyl-7-(4-Benzyl-piperazin-1-yl)-5-fluorobenzofuran-2-carboxylate

https://huagongshe.com/ja/reaction/383849

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物1-BenzylpiperazineHCID 75994—
反応物Binap, (A+-)-HCID 634876—
反応物Ethyl 7-bromo-5-fluorobenzofuran-2-carboxylateHCID 59636759—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物Ethyl-7-(4-Benzyl-piperazin-1-yl)-5-fluorobenzofuran-2-carboxylateHCID 59636706—

反応手順

Benzylpiperazine (1.3 mL, 8.4 mmol), BINAP (0.43 g, 0.69 mmol), Pd2 dba3 (0.32 g, 0.35 mmol), cesium carbonate (3.25 g, 9.76 mmol) were added to a degassed solution of 7-bromo-5-fluoro-benzofuran-2-carboxylic acid ethyl ester (2.0 g, 6.97 mmol) in toluene (50 mL). The mixture was heated at reflux over night. After cooling, the mixture was filtered through a pad of celite and washed with dichloromethane. The filtrate was concentrated under reduced pressure. The product was purified by flash chromatography (SiO2; hexane/EtOAc, 7/3). Yield: 1.6 g (60%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08367676B2
出典データセットuspto-grants-2013_02
ORD IDord-7d7011b0e5ec43758af116dea5115726
出典メモuspto-grants-2013_02