In summary, this highly efficient protocol developed by Chen et al. represents a remarkable success of applying C–H activation strategy to convert complex linear peptides to challenging constrained macrocycles, solving the long standing issue of size- and composition-dependence in such events. This methodology should greatly accelerate the access to a diverse collection of novel macrocyclic structures, which should be of great value in the survey of promising lead compounds for the development of peptide-based therapeutics.
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