Green Organocatalysis as a Sustainable Platform for Drug Synthesis: A Perspective

Abstract

Organocatalysis, which provides metal‐free, effective, and highly selective transformations in line with green chemistry principles, has emerged as a sustainable method in pharmaceutical synthesis. This review highlights the fundamental concepts of organocatalysis, including catalyst types, activation modes, and environmentally safe reaction conditions like aqueous media, deep eutectic solvents, ionic liquids, mechanochemistry, and solvent‐free procedures. Efficiency, scalability, and environmental performance have been further improved by combining organocatalysis with complementary green technologies like photoorganocatalysis, chemoenzymatic cascades, and recyclable catalysts. Important uses in drug synthesis are covered, with a focus on asymmetric transformations through enamine and iminium ion pathways that are related to antiviral, anticancer, and nitrogen‐containing heterocyclic drugs as well as chiral building blocks. Aldol, Michael, C─N bond‐forming, and cycloaddition processes are among the fundamental organocatalytic reactions that are discussed along with their application in continuous‐flow systems. Overall, a strong and sustainable framework to produce next‐generation drugs is presented by the convergence of green organocatalysis with advanced reaction media.