Regioselective Hydroarylations and Parallel Kinetic Resolution of Vince Lactam

摘要

Modular small-molecule motifs that induce or mimic loop and turn secondary structure are important for the design of peptide-based drugs. Incorporation of nonnatural structures into otherwise natural peptides can lead to favorable pharmacokinetic properties, such as increased cell permeability and oral bioavailability, and is a prominent feature of successful pharmaceuticals, such as telaprevir and bocepre-vir. In the field of peptidomimetics and foldamers, oligomers containing γ-amino acids can form stabilized secondary structures, can be resistant to serum and tissue proteases, and can bind to biological macromolecules.