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HRID 2263192作成日:2026年10月26日

Water → N-(3,4-Dimethylisoxazol-5-yl)-4-[4-(4-fluorophenyl)-1,3-thiazol-2-yl]piperazine-1-carboxamide

https://huagongshe.com/reaction/2263192

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-(4-Fluorophenyl)-2-thiazolyl]piperazineHCID 8027201—
反応物HCID 86245257HCID 86245257—
溶媒Dimethyl SulfoxideHCID 679—
生成物N-(3,4-Dimethylisoxazol-5-yl)-4-[4-(4-fluorophenyl)-1,3-thiazol-2-yl]piperazine-1-carboxamideHCID 6877629450.2%

反応条件

温度70 °C

反応手順

A mixture of 2,2,2-trichloroethyl (3,4-dimethylisoxazol-5-yl)carbamate (240 mg, 0.834 mmol), 1-[4-(4-fluorophenyl)-1,3-thiazol-2-yl]piperazine (200 mg, 0.760 mmol) and diisopropylethylamine (0.265 ml, 1.52 mmol) in dimethylsulfoxide (2.5 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 recrystallized from a mixed solvent of hexane and tetrahydrofuran to give the desired product (153 mg, 50.2%) 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-15f35b7610864667b01816b72ddcb72f
出典メモuspto-grants-2010_12