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HRID 2263173作成日:2026年10月26日

Water → N-[6-(Acetylamino)pyridin-3-yl]-4-(5-methyl-4-phenyl-1,3-thiazol-2-yl)piperazine-1-carboxamide

https://huagongshe.com/reaction/2263173

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5-Methyl-4-phenyl-2-piperazinyl-1,3-thiazoleHCID 17233868—
反応物2,2,2-Trichloroethyl[6-(acetylamino)pyridin-3-yl]carbamateHCID 86245259—
溶媒Dimethyl SulfoxideHCID 679—
生成物N-[6-(Acetylamino)pyridin-3-yl]-4-(5-methyl-4-phenyl-1,3-thiazol-2-yl)piperazine-1-carboxamideHCID 6877944647.8%

反応条件

温度70 °C

反応手順

A mixture of 2,2,2-trichloroethyl [6-(acetylamino)pyridin-3-yl]carbamate (277 mg, 0.848 mmol), 1-(5-methyl-4-phenyl-1,3-thiazol-2-yl)piperazine (200 mg, 0.771 mmol) and diisopropylethylamine (0.148 ml, 0.848 mmol) in dimethylsulfoxide (2.6 ml) was stirred at 70° C. for 18 hours. Water was poured into the reaction solution, and the mixture was extracted with ethyl acetate. The extract was washed with water and dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate) and recrystallized from a mixed solvent of hexane and tetrahydrofuran to give 161 mg (47.8%) of the desired product as a solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07851473B2
出典データセットuspto-grants-2010_12
ORD IDord-37c81f786d24455b9f77d935f0c91186
出典メモuspto-grants-2010_12