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✖-(Protected α-aminoacyl) benzotriazoles are efficient acylating reagents that offer many advantages in the preparation of peptides and their mimetics and conMugates. Advances in methodology, made possible by these novel reagents, have given rise to solution-and solid-phase preparative techniques for generating complex peptides and peptide conMugates, which are useful in the construction of diverse libraries of building blocks for medicinal chemistry.