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HRID 83617作成日:2026年10月26日

1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)-N-(2-(pyridin-4-yl)ethyl)piperidine-4-carboxamide

https://huagongshe.com/reaction/83617

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1-HydroxybenzotriazoleHCID 75771—
反応物DiisopropylethylamineHCID 81531—
反応物4-PyridineethanamineHCID 83275—
反応物1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acidHCID 57385796—
溶媒DichloromethaneHCID 6344—
生成物1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)-N-(2-(pyridin-4-yl)ethyl)piperidine-4-carboxamideHCID 66571217—

反応手順

1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acid (390 mg, 0.982 mmol), 1-hydroxybenzotriazole (221 mg, 1.637 mmol) and EDCI (314 mg, 1.637 mmol) were dissolved in DCM (Volume: 4.0 ml). The suspension was stirred at room temperature for 10 minutes where it turned clear. Hunig's Base (0.286 ml, 1.637 mmol) and 2-(pyridin-4-yl)ethanamine (0.098 ml, 0.819 mmol) were added. The reaction was stirred at room temperature overnight. The reaction was concentrated and triturated with ethyl acetate to afford the product as a white solid. Yield: 328 mg (White solid) 1H-NMR (500 MHz, DMSO-d6) 8.46, 7.91, 7.63, 7.55, 7.34, 7.25-7.18, 7.14-7.06, 6.72, 5.49, 4.54-3.80, 3.32, 3.07-2.77, 2.73, 2.37-2.28, 1.77-1.18.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846684B2
出典データセットuspto-grants-2014_09
ORD IDord-df94553b86184979bf7350a0e906575b
出典メモuspto-grants-2014_09