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HRID 447803作成日:2026年10月25日

Water → 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide hydrochloride

https://huagongshe.com/reaction/447803

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物DiisopropylethylamineHCID 81531—
反応物2-Cyano-2-(3,4-dichloro-5(2H)-oxo-2-furyl)acetamideHCID 541792—
反応物1-[5-Chloro-2-(methylsulfonyl)phenyl]methanamine hydrochlorideHCID 66969896—
溶媒EthanolHCID 702—
生成物5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide hydrochlorideHCID 6697008689.9%

反応条件

温度70 °C

反応手順

(Step 4) To a suspension of 2-cyano-2-(3,4-dichloro-5-oxo-2,5-dihydrofuran-2-yl)acetamide (0.28 g) and 1-[5-chloro-2-(methylsulfonyl)phenyl]methanamine hydrochloride obtained in Step 3 (0.26 g) in ethanol (3 ml) was added N,N-diisopropylethylamine (0.44 ml) at room temperature, and the resulting mixture was heated under reflux for 4 hr. The reaction mixture was treated with water and stirred at 70° C. for 1 hr. After cooling to room temperature, the precipitate was collected by filtration and dried. The precipitate was suspended in methanol, and treated with a 2 M hydrogen chloride-methanol solution (0.3 ml). The resulting mixture was stirred at room temperature overnight. The precipitate was collected by filtration and dried to give the title compound (0.22 g) as white crystals.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08481569B2
出典データセットuspto-grants-2013_07
ORD IDord-56ed163206734d0fbcd7db865f382310
出典メモuspto-grants-2013_07