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HRID 2263264作成日:2026年10月24日

Water → 4-[4-(2,3-difluorophenyl)-1,3-thiazol-2-yl]-N-pyridin-3-ylpiperazine-1-carboxamide

https://huagongshe.com/ja/reaction/2263264

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HCID 68575380HCID 68575380—
反応物1-[4-(2,3-Difluorophenyl)-1,3-thiazol-2-yl]piperazineHCID 68776289—
溶媒Dimethyl SulfoxideHCID 679—
生成物4-[4-(2,3-difluorophenyl)-1,3-thiazol-2-yl]-N-pyridin-3-ylpiperazine-1-carboxamideHCID 1158942655%

反応条件

温度70 °C

反応手順

A mixture of 2,2,2-trichloroethyl pyridin-3-ylcarbamate (211 mg, 0.782 mmol), 1-[4-(2,3-difluorophenyl)-1,3-thiazol-2-yl]piperazine (200 mg, 0.711 mmol) and diisopropylethylamine (0.248 ml, 1.42 mmol) in dimethyl sulfoxide (2.5 ml) was stirred at 70° C. for 15 hours. Water was poured to 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 give 157 mg (55.0%) of the desired product as a solid. mp 172-173° C.

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-cb1c431329fe4aba86706b1fb07ddfe3
出典メモuspto-grants-2010_12