Herein is described the chemoselective Cu (II)-HOBt promoted chemical ligation of glycosylamines and peptide thioacids to give N-glycosylated peptides. The method is distinguished from other chemical approaches to peptide N-glycosylation in that (1) it can be employed in the presence of unprotected N-terminal and Lys side chain amines;(2) it is remarkably fast, going to completion in under 30 min; and (3) it produces glycopeptides ...