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HRID 1280974作成日:2026年10月25日

1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 2-((N-benzoylleucyl)aminomethyl)-1-(4-chlorobenzyl)pyrrolidine

https://huagongshe.com/reaction/1280974

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Benzoyl-L-leucineHCID 853887—
反応物2-(Aminomethyl)-1-(4-chlorobenzyl)pyrrolidineHCID 14709036—
溶媒ChloroformHCID 6212—
溶媒DichloromethaneHCID 6344—
溶媒TriethylamineHCID 8471—
生成物2-((N-benzoylleucyl)aminomethyl)-1-(4-chlorobenzyl)pyrrolidineHCID 53639429—

反応条件

温度25 °C

反応手順

A solution of 2-(aminomethyl)-1-(4-chlorobenzyl)pyrrolidine (22.5 mg, 0.10 mmol) and dl-benzoylleucine (0.12 mmol) in CHCl3 (1 mL) was treated with EDCI (23 mg), HOBt (16.2 mg) and Et3N (15.2 μL), and stirred at 25° C. for 16 h. The reaction mixture was diluted with CH2Cl2 (0.5 mL), washed with 2 N aqueous NaOH solution (2×0.75 mL), dried by filtration through a PTFE membrane and concentrated to afford 2-{(N-benzoylleucyl)aminomethyl}-1-(4-chlorobenzyl)pyrrolidine (compound No. 344) (74 mg, quant): The purity was determined by RPLC/MS (85%); ESI/MS m/e 442 (M++H, C25H32ClN3O2).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06451842B1
出典データセットuspto-grants-2002_09
ORD IDord-8a0de64a23794320bf34e4ed8f6f384a
出典メモuspto-grants-2002_09