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HRID 76386作成日:2026年10月25日

Dichloromethane → 3-(5-(5-Acetylthiophen-2-yl)nicotinoyl)-1-methylpyrrolidin-2-one

https://huagongshe.com/reaction/76386

反応式

関与物質

役割名称HCID仕込み量
反応物DichloromethaneHCID 6344—
反応物(5-Acetylthiophen-2-yl)boronic acidHCID 4143377—
反応物3-(5-Bromopyridine-3-carbonyl)-1-methylpyrrolidin-2-oneHCID 14061371—
触媒Ferrocene-1,1'-bis-(diphenylphosphine)HCID 635956—
溶媒Dioxane tolueneHCID 21840791—
生成物3-(5-(5-Acetylthiophen-2-yl)nicotinoyl)-1-methylpyrrolidin-2-oneHCID 7157011850%

反応条件

温度85 °C

反応手順

A mixture of 3-(5-bromonicotinoyl)-1-methylpyrrolidin-2-one 3 (1 equiv), 5-Acetyl-2-thiopheneboronic acid (1.2 equiv), 1,1′-bis(diphenylphosphino)ferrocene]dichloro palladium(II) complex with DCM (0.1 equiv) and 2M Na2CO3(4 equiv) in toluene/1,4-dioxane(4:1, 15 volumes) was degassed and filled with nitrogen. Then the reaction mixture was heated to 85° C. and maintained for 2 h. After completion of the reaction filtered through Celite bed and washed with ethyl acetate. The combined organic layer was dried over with anhydrous sodium sulfate, filtered and concentrated under reduced pressure to obtain crude residue which was purified by silica-gel column chromatography using 2% MeOH/DCM as an eluent to afford 50% yield of titled compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08835640B1
出典データセットuspto-grants-2014_09
ORD IDord-bee8575046a648daae173e0b9e6482e5
出典メモuspto-grants-2014_09