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HRID 83622作成日:2026年10月26日

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

https://huagongshe.com/reaction/83622

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3-MethoxyphenethylamineHCID 74866—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物DiisopropylethylamineHCID 81531—
反応物1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acidHCID 57385796—
溶媒WaterHCID 962—
溶媒DichloromethaneHCID 6344—
溶媒Ethyl AcetateHCID 8857—
生成物1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)-N-(3-methoxyphenethyl)piperidine-4-carboxamideHCID 66571277—

反応手順

1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acid (100 mg, 0.252 mmol), 1-hydroxybenzotriazole (51.1 mg, 0.378 mmol), and EDCI (72.5 mg, 0.378 mmol) were dissolved in 2.0 mL of DCM. The reaction was allowed to stir at room temperature for 10 minutes before 2-(3-methoxyphenyl)ethanamine (0.056 ml, 0.378 mmol) and Hunig's Base (0.066 ml, 0.378 mmol) were added as a 1.0 mL DCM solution. The reaction was allowed to stir overnight. The reaction was diluted with water and ethyl acetate. The organic phase was washed with 1N HCl, saturated sodium bicarbonate, and brine. The organic phase was dried over magnesium sulfate, filtered, and concentrated. The crude material was triturated with ethyl acetate to obtain product as a white solid. (Yield: 89 mg, white solid)

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-7b0e70d032224d87ab12c94bc19d265a
出典メモuspto-grants-2014_09