at Peking University School of Pharmaceutical Sciences
​​​​the dong research group
5. Shape linear peptides into rigid rings: a sp3 C–H arylation approach to cyclophane-braced peptide macrocycles
Sci. China Chem. 2018, 61, 1477.
Yuankun Dao, Suwei Dong*

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.