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HRID 872991作成日:2026年10月25日

1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → N-(4-((2-aminopyridin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide

https://huagongshe.com/reaction/872991

反応式

関与物質

役割名称HCID仕込み量
反応物1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 15908—
反応物HOAtHCID 181649—
反応物Antipyric acidHCID 246564—
反応物HCID 22936741HCID 22936741—
溶媒DichloromethaneHCID 6344—
生成物N-(4-((2-aminopyridin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamideHCID 7305360853%

反応条件

温度45 °C

反応手順

To a mixture of 4-(4-aminophenoxy)pyridin-2-amine (101 mg, 0.5 mmol) and 1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid (118 mg, 0.51 mmol) in DCM (5 mL) was added EDCI (115 mg, 0.6 mmol) and HOAT (13.6 mg, 0.1 mmol). The reaction was stirred at 45° C. for 3 hours, and then quenched with water (20 mL). The organic phase was separated and concentrated in vacuo. The residue was purified by a silica gel column chromatography (DCM/CH3OH (v/v)=20/1) to give the title compound as a light grey solid (110 mg, 49.2%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08975282B2
出典データセットuspto-grants-2015_03
ORD IDord-9f3396a414114ac386a622f1ebbd5907
出典メモuspto-grants-2015_03