Synthesis of 3-Substituted Pyrrolidines via Palladium-Catalysed Hydroarylation

Abstract

Metal-catalysed reactions have revolutionised synthetic chemistry, allowing access to unprecedented molecular architectures with powerful properties and activities. Nonetheless, some transformations remain sparse in number, or out of reach, even with the diverse modern catalytic chemical arsenal, including bimolecular alkene hydroarylation reactions. We report here the first palladium-catalysed alkene hydroarylation to give 3-aryl pyrrolidines, a class of small molecule with potency in a diverse range of biological scenarios. The process has broad substrate scope and can be used to directly deliver drug-like molecules in a single step from readily available precursors.