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HRID 70543作成日:2026年10月25日

Water → (5R)-5-[(4-tert-butylphenyl)ethynyl]-1-(2,4-dimethoxybenzyl)pyrrolidin-2-one

https://huagongshe.com/reaction/70543

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物1-tert-Butyl-4-iodobenzeneHCID 142029—
反応物(5R)-1-(2,4-Dimethoxybenzyl)-5-ethynylpyrrolidin-2-oneHCID 58452699—
触媒Copper iodideHCID 83717—
触媒HCID 178418476HCID 178418476—
溶媒TriethylamineHCID 8471—
生成物(5R)-5-[(4-tert-butylphenyl)ethynyl]-1-(2,4-dimethoxybenzyl)pyrrolidin-2-oneHCID 6739860984%

反応手順

Copper iodide (74 mg) and bis(triphenylphosphine)palladium(II) dichloride (135 mg) were added to a solution of 4-tert-butyliodobenzene (3.0 g) in triethylamine (10 mL), and the mixture was stirred at room temperature for 15 minutes. (5R)-1-(2,4-Dimethoxybenzyl)-5-ethynylpyrrolidin-2-one (1.0 g) was added thereto over one hour, and the mixture was stirred at room temperature for three hours. The reaction solution was poured into water, followed by extraction with ethyl acetate. The organic layer was washed with brine, dried over anhydrous magnesium sulfate and filtered. The solvent was then evaporated under reduced pressure. The residue was purified by silica gel column chromatography (hexane:ethyl acetate=1:0→1:1) to give (5R)-5-[(4-tert-butylphenyl)ethynyl]-1-(2,4-dimethoxybenzyl)pyrrolidin-2-one as a colorless powder (1.25 g, 84%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08822503B2
出典データセットuspto-grants-2014_09
ORD IDord-b87af4f26a1349cb8f1f91571641531d
出典メモuspto-grants-2014_09