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HRID 2263294作成日:2026年10月26日

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

https://huagongshe.com/reaction/2263294

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-(2,4-Difluorophenyl)-1,3-thiazol-2-yl]piperazineHCID 61779838—
反応物2,2,2-Trichloroethyl pyridazin-3-ylcarbamateHCID 68576698—
溶媒Dimethyl SulfoxideHCID 679—
生成物4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-pyridazin-3-ylpiperazine-1-carboxamideHCID 6877962347.5%

反応条件

温度70 °C

反応手順

A mixture of 2,2,2-trichloroethyl pyridazin-3-ylcarbamate (212 mg, 0.782 mmol), 1-[4-(2,4-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 3 days. 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 136 mg (47.4%) 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-a63d64f1c70349f7a437e363b86e3921
出典メモuspto-grants-2010_12