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HRID 1838340作成日:2026年10月25日

Water → 2-(2-Tetrahydrofuranyl)-5-methanesulfonyl-1-benzenesulfonylindole

https://huagongshe.com/reaction/1838340

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物TriethylamineHCID 8471—
反応物2-EthynyloxolaneHCID 10034582—
反応物1-Benzenesulfonylamino-2-iodo-4-methanesulfonylbenzeneHCID 22504376—
溶媒1,4-DioxaneHCID 31275—
生成物2-(2-Tetrahydrofuranyl)-5-methanesulfonyl-1-benzenesulfonylindoleHCID 2250444991.8%

反応条件

温度60 °C

反応手順

To a solution of 1-benzenesulfonylamino-2-iodo-4-methanesulfonylbenzene (256 mg) in 1,4-dioxane (6 ml), 2-ethynyltetrahydrofuran (169 mg), bistriphenylphosphine palladium dichloride (21 mg), cuprous iodide (11 mg) and triethylamine (89 mg) were added successively and the mixture was stirred in a sealed tube at 60° C. for 3 hours. After cooling, the reaction solution was poured into water, extracted with dichloromethane, dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The resulting residue was separated using silica gel preparative thin-layer chromatography (hexane:ethyl acetate=1:1) to obtain 218 mg of the desired product in a white amorphous form.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06673797B1
出典データセットuspto-grants-2004_01
ORD IDord-69ea4f2f131c4410be81dd751da3a87c
出典メモuspto-grants-2004_01