Solid‐Phase Synthesis of Peptidomimetics with Peptide Backbone Modifications

Peptidomimetics are a class of compounds with promising pharmacological properties. Peptidomimetics reduce limitations of peptides including low bioavailability, poor stability, and poor cell‐permeability. Peptide backbone modifications are a frequently used manipulation to reach desirable properties of the peptide molecules. The development of accessible synthetic methodologies plays an important role in peptidomimetic progress. Synthesis of peptidomimetics proceeds via solution and solid‐phase synthesis strategies. Solid‐phase organic synthesis serves as a powerful tool for the preparation of peptidomimetic molecules, thus, numerous strategies have been developed over the years. In this review, we discuss solid‐phase synthetic approaches for peptide backbone modifications that were presented in the last two decades.