Harnessing Organocatalysis for Enantioselective Chromane Synthesis

Chromanes are privileged scaffolds in medicinal chemistry because they exhibit diverse biological activities. Their stereoselective synthesis has become a critical objective in drug development. The emergence of organocatalysis has sparked a paradigm shift in synthetic chemistry by offering a highly selective alternative to traditional metal-catalyzed reactions. This review discusses the transformative impact of organocatalyzed reactions on the asymmetric synthesis of chromane derivatives, focusing on key classes of catalysts such as chiral phosphoric acid, chiral amines, bifunctional systems, and others reported since 2020. Organocatalysis not only achieves high levels of stereocontrol but also adheres to the principles of green chemistry by eliminating toxic metals and enabling mild reaction conditions. These advancements diversify synthetic methodologies and establish organocatalysis as a fundamental approach in the sustainable synthesis of bioactive chromanes.