Macrocyclic Peptidomimetics Prepared by Ring-Closing Metathesis and Azide-Alkyne Cycloaddition

Macrocycles are finding increasing use as a means to define the backbone geometries of peptides and peptidomimetics. Ring-closing metathesis and CuI-catalyzed azide-alkyne cycloaddition are particularly useful for introducing such rings and they do so in high yield and with a good functional group tolerance and compatibility. Here, we present an overview of the use of these two methods, with reference to selected examples and particular reference to β-strand peptidomimetics for use as protease inhibitors.