A synthetic route to enediyne-bridged amino acids

A general strategy for the preparation of enediyne-bridged amino acids has been disclosed. A cross-coupling reaction between amino- and carboxyl-modified amino acids under Sonogashira reaction conditions gave a protected enediyne–peptide conjugate. The model obtained can be used as a template in studies of Bergman cycloaromatization or peptide conformational preferences induced by the presence of the enediyne moiety.