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HRID 2146作成日:2026年10月24日

Triethylamine → 2-(3,4-Dimethoxybenzenesulphonyl)-4-(2-pyrid-2-ylethynyl)isoindoline

https://huagongshe.com/ja/reaction/2146

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物EthynylpyridineHCID 137268—
反応物2-(3,4-Dimethoxybenzenesulphonyl)-4-bromoisoindolineHCID 19689661—
触媒PalladiumHCID 23938—
触媒Dichlorobis(triphenylphosphine)palladiumHCID 6102075—
溶媒DimethylformamideHCID 6228—
溶媒Ethyl AcetateHCID 8857—
生成物2-(3,4-Dimethoxybenzenesulphonyl)-4-(2-pyrid-2-ylethynyl)isoindolineHCID 1968964012.5%

反応条件

温度90 °C

反応手順

2-(3,4-Dimethoxybenzenesulphonyl)-4-bromoisoindoline (0.19 g), triethylamine (0.10 ml), 2-ethynylpyridine(0.06 g) and bis (triphenylphosphine)palladium(II)chloride (10%) in anhydrous N,N-dimethylformamide(2 ml) were stirred together under an inert atmosphere and heated to 90° C. After 20 hours further 2-ethynylpyridine(0.12 g) and palladium catalyst (20%) were added and heating continued for 3 days. The reaction mixture at room temperature was diluted with ethyl acetate, filtered through a pad of silica and the filtrate evaporated in vacuo to yield a yellow residue. Purification by column chromatography, eluting with a 20-100% ethyl acetate in hexane gradient afforded the title compound (25 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05728712
出典データセットuspto-grants-1998_03
ORD IDord-1fbe8bec2d7a4b37b8e811f839c2b36c
出典メモuspto-grants-1998_03