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HRID 2263140作成日:2026年10月25日

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

https://huagongshe.com/reaction/2263140

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1-(4-Phenyl-1,3-thiazol-2-yl)piperazineHCID 712468—
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-(4-phenyl-1,3-thiazol-2-yl)piperazine-1-carboxamideHCID 6877965313.7%

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 (293 mg, 0.897 mmol), 1-(4-phenyl-1,3-thiazol-2-yl)piperazine (200 mg, 0.815 mmol) and diisopropylethylamine (0.156 ml, 0.897 mmol) in dimethylsulfoxide (2.7 ml) was stirred at 70° C. for 15 hours. Water was poured into the reaction mixture 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 obtain the desired product (47.3 mg, 13.7%) 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-28ddafc44ba942d0ad509f83d5ab655e
出典メモuspto-grants-2010_12