Macrocycle Compounds

Growing interest towards medium- and large-sized macrocycles closely linked with the field of protein-protein interactions (PPI) as promising therapeutic targets. Pharmaceutical companies utilized two methodologies for the design and synthesis of a macrocyclic peptidomimetic library.

The first methodology involves ring expansion using the Bormann-Wasserman strategy (BWS), allowing for the synthesis of 10-12-membered lactams. This approach provides access to unique functionally enriched, spiro and fused scaffolds.

The second methodology is based on click-macrocyclization of linear peptidomimetics that bear acetylene and azide functionalities at the ends. This method enables the production of 14-22 membered macrocyclic peptidomimetics.

As a result, we have obtained a novel, IP clean, and diverse set of macrocyclic scaffolds. These scaffolds are now available for the synthesis proposal.