Ring-Closing Metathesis in Pharmaceutical Development: Fundamentals, Applications, and Future Directions

Abstract

Ring-closing metathesis (RCM) has become indispensable in organic synthesis for both academic investigations and industrial applications. This review provides an overview of RCM reactions, focusing on the practical aspects that researchers in an industrial environment may find of interest. Key elements of reaction design and lessons learned from these applications are discussed to help those considering implementing RCM reactions on scale, particularly in manufacturing active pharmaceutical ingredients (APIs). Advances in the development of more effective catalysts and new methodologies, such as enantioselective RCM and stereoselective macrocyclic RCM, are also briefly discussed.