Merging DOS with LSF: a simple pathway toward constrained peptidomimetics,

Making a precise nonacidic C-H bond reacting allows to generate a site of functionalization otherwise unexploitable. Many substrates, including amino acids, have been employed in TM-assisted C-H bond activation reactions, exploiting the use of Directing Groups to achieve chemoselectivity. We combined the DOS-compatible Castagnoli-Cushman Reaction with Pd-catalyzed C(sp3)-H bond activation reaction, and we developed a range of heterocyclic arylated peptidomimetics.