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HRID 1158718作成日:2026年10月27日

Toluene → 1-[3-(3-Thienyl)phenyl]piperazine

https://huagongshe.com/reaction/1158718

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Thiophene-3-boronic acidHCID 581760—
反応物1-(3-Bromophenyl)piperazineHCID 2757154—
触媒HCID 178418397HCID 178418397—
溶媒WaterHCID 962—
生成物1-[3-(3-Thienyl)phenyl]piperazineHCID 5898514083.8%

反応手順

A mixed solution of 1-(3-bromophenyl)-piperazine (300 mg, 1.24 mmol), 3-thienylboronic acid (239 mg, 1.87 mmol), tetrakis(triphenylphosphine)palladium (173 mg, 0.149 mmol), 2N aqueous solution of sodium carbonate (4.98 ml, 9.95 mmol), and toluene (12 ml) was stirred at 95° C. for 15 hours under a nitrogen atmosphere. After cooling to room temperature, water was poured into the reaction solution, and extracted with ethyl acetate. The extract was washed with water, dried over anhydrous magnesium sulfate, and the solvent was distilled away under reduce pressure. The residue was purified by basic silica gel column chromatography (ethyl acetate) to give the titled compound 254 mg (83.5%) as an oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07812025B2
出典データセットuspto-grants-2010_10
ORD IDord-a3460c4451564704923857d88a360514
出典メモuspto-grants-2010_10