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HRID 1814113作成日:2026年10月24日

Water → 6-(1-Benzenesulfonyl-5-methylthio-1h-pyrrolo[2,3-b]pyridin-2-yl)nicotinic acid ethyl ester

https://huagongshe.com/ja/reaction/1814113

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Potassium AcetateHCID 517044—
反応物2-Benzenesulfonylamino-3-iodo-5-methylthiopyridineHCID 15486851—
反応物5-Ethoxycarbonyl-2-trimethylsilylethynylpyridineHCID 22504397—
溶媒1,4-DioxaneHCID 31275—
生成物6-(1-Benzenesulfonyl-5-methylthio-1h-pyrrolo[2,3-b]pyridin-2-yl)nicotinic acid ethyl esterHCID 6844473998.5%

反応条件

温度100 °C

反応手順

To a solution of 2-benzenesulfonylamino-5-methylthio-3-iodo-pyridine (100 mg) in 1,4-dioxane (2.5 ml), 5-ethoxycarbonyl-2-trimethylsilylethynylpyridine (185 mg), bistriphenylphosphine palladium dichloride (9 mg), cuprous iodide (5 mg) and potassium acetate (37 mg) were added successively and the mixture was stirred in a sealed tube at 100° C. for 15 hours. After cooling, the reaction solution was poured into water, extracted with ethyl acetate, 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=2:1) to obtain 110 mg of the desired product as an orange oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06875770B2
出典データセットuspto-grants-2005_04
ORD IDord-0f1fd7e7c0f54fbc91234c3ff00dc5b1
出典メモuspto-grants-2005_04