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HRID 251373作成日:2026年10月27日

1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 5-amino-1-(5-cyclopropylcarbamoyl-2-methylphenyl)-1H-pyrazole-4-carboxylic acid (2-methylcyclohexyl)-amide

https://huagongshe.com/reaction/251373

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2-MethylcyclohexylamineHCID 23432—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物5-amino-1-(5-cyclopropylcarbamoyl-2-methylphenyl)-1H-pyrazole-4-carboxylic acidHCID 58088954—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
生成物5-amino-1-(5-cyclopropylcarbamoyl-2-methylphenyl)-1H-pyrazole-4-carboxylic acid (2-methylcyclohexyl)-amideHCID 1174979670%

反応手順

A solution of 5-amino-1-(5-cyclopropylcarbamoyl-2-methylphenyl)-1H-pyrazole-4-carboxylic acid (21 mg), 2-methylcyclohexylamine (10 mg), EDCI (28 mg) and HOBt (12 mg) in DMF (0.75 ml) was reacted at room temperature for 24 h. Water (4 ml) was added and the solution was extracted with ethyl acetate (3 mL ×2). The organic phase was then washed with water (3 mL), dried over Na2SO4 and evaporated. The residue was purified by preparative TLC plate to give the desired product 5-amino-1-(5-cyclopropylcarbamoyl-2-methylphenyl)-1H-pyrazole-4-carboxylic acid (2-methylcyclohexyl)-amide (19 mg, 70%). HPLC (4 minute gradient) tR 2.34 min; MS m/z 396.31 [M+H]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07863314B2
出典データセットuspto-grants-2011_01
ORD IDord-1ce963fc4d25473b9ef51ec57da92997
出典メモuspto-grants-2011_01