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HRID 80203作成日:2026年10月25日

Methanol → 1-(4-Methylpyridin-3-yl)-3-(4-methylthieno[3,2-e]pyridin-2-yl)imidazolidin-2-one

https://huagongshe.com/reaction/80203

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物Potassium CarbonateHCID 11430—
反応物Methylboronic AcidHCID 139377—
反応物1-(4-Chloro-thieno[3,2-c]pyridin-2-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-oneHCID 49871870—
触媒Tetrakis(triphenylphosphine)palladiumHCID 11979704—
溶媒ChloroformHCID 6212—
生成物1-(4-Methylpyridin-3-yl)-3-(4-methylthieno[3,2-e]pyridin-2-yl)imidazolidin-2-oneHCID 6878264916.39%

反応手順

Tetrakis (triphenylphosphine) palladium (33 mg, 0.0288 mmol) was added to potassium carbonate (120 mg, 0.8649 mmol) previously purged with argon (30 minutes). The reaction mixture was purged with argon for 15 minutes, followed by the addition of 1-(4-chloro-thieno[3,2-c]pyridin-2-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (98A: 100 mg, 0.2883 mmol) and methyl boronic acid (21 mg, 0.3459 mmol). The reaction mixture was heated to reflux for 6 hours. The reaction was monitored by TLC (10% MeOH in CHCl3). The reaction mixture was concentrated to afford the crude product. Purification by column chromatography on silica gel (3-4% MeOH in CHCl3), followed by preparative HPLC afforded 10 mg of the product (16.39% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号USRE045173E1
出典データセットuspto-grants-2014_09
ORD IDord-d1ef7f24fe0c4034b7ba44cc299852fa
出典メモuspto-grants-2014_09