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HRID 133572作成日:2026年10月26日

1-Hydroxybenzotriazole → 2-((N-benzoylleucyl)aminomethyl)-1-(4-chlorobenzyl)pyrrolidine

https://huagongshe.com/reaction/133572

反応式

関与物質

役割名称HCID仕込み量
反応物1-HydroxybenzotriazoleHCID 75771—
反応物Benzoyl-L-leucineHCID 853887—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
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

EDCl (23 mg), HOBt (16.2 mg) and triethylamine (15.2 μL) were added to a chloroform (1 mL) solution of 2-(aminomethyl)-1-(4-chlorobenzyl)pyrrolidine (22.5 mg, 0.10 mmol) and dl-benzoylleucine (0.12 mL), and the resulting mixture was stirred at 25° C. for 16 hours. The reaction mixture was diluted with dichloromethane (0.5 mL), washed with a 2 M aqueous solution of NaOH (0.75 mL×2), filtered through a PTFE membrane, thereby dried and concentrated to provide 2-[(N-benzoylleucyl)aminomethyl]-1-(4-chlorobenzyl)pyrrolidine (Compd. No. 344) (74 mg, quantitative). The purity was determined by RPLC/MS (85%). ESI/MS m/e 442 (M++H, C23H32ClN3O2).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07390830B1
出典データセットuspto-grants-2008_06
ORD IDord-a7466de645af45ffb3bc6e7d7e745a01
出典メモuspto-grants-2008_06