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

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

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).

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