Synthesis of biologically active compounds is of paramount importance to the biomedical sciences for the development of novel therapeutic agents. Such substances often feature various types of unique and complex structures, which make them challenging targets for synthetic efforts. Their total synthesis offers the chance to implement the use of newly developed, efficient and highly selective synthetic procedures and/or strategies in a complex environment. In this respect, thanks to the development of increasingly efficient molybdenum and ruthenium catalysts, olefin metathesis is now an integral part of modern synthetic methods. This review article will highlight with selected examples from the recent literature assets and limitations of the olefin metathesis reaction in the synthesis of biologically active compounds.
Keywords: Cross-metathesis, Natural products, Olefin metathesis, Relay ring-closing metathesis, Ring-closing metathesis, Ruthenium catalysts, Tandem olefin metathesis, Temporary tethered olefin metathesis.