1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI×HCl)

Abstract

(A) Conjugation of acids with aromatic amines generally leads to poor yields of amides. However, when performed with EDCI•HCl,coupling between an acid and an amine with low nucleophilicity yields 83% of the product. 4 (B) In the penultimate step of the total synthesis of iso-duocarmycin SA, direct coupling of the secondary amine with the corresponding acid using EDCI•HCl afforded 82% of the product in 30 minutes without any racemization.5 © Georg Thieme Verlag Stuttgart New York.