Abstract
The concept of site-specific integration of fragments into macrocyclic entities has not yet found application in the realm of synthetic chemistry. Here we show that the reduced amidicity of aziridine amide bonds provides an entry point for the site-specific integration of amino acids and peptide fragments into the homodetic cyclic peptide architecture. This new synthetic operation improves both the convergence and divergence of cyclic peptide synthesis.
Supporting Information
Experimental details, optimization data, characterization data, HPLC traces, and 1H and 13C NMR spectra of all new compounds. This material is available free of charge via the Internet at http://pubs.acs.org.
