Recent Advancements on the Povarov Reactions for the Synthesis of Quinolines and Tetrahydroquinolines

Abstract The Povarov reaction is a highly efficient method for synthesizing tetrahydroquinolines (THQs) and quinolines (QUINs), which are significant heterocyclic scaffolds in many bioactive compounds. This mini‐review emphasizes recent advancements in the Povarov reaction, a one‐pot multicomponent reaction (MCR) that facilitates the synthesis of functionalized quinolines, tetrahydroquinolines, and related compounds. This reaction, which involves aniline, aldehydes, and olefins, is highly relevant to synthetic chemists and aligns with green chemistry principles. Initially described as a pericyclic reaction, the Povarov reaction involves cycloaddition between an imine and an alkene. The popularity of Povarov reaction has surged, particularly when the imine is generated in situ through the reaction of arylamines and aldehydes, followed by cyclization with alkenes. The advantages of this methodology compared to conventional methods are carefully analyzed at the end of this paper. This approach not only enhances the efficiency of the synthesis process but also creates opportunities to explore a wide range of chemical reactions and pathways, in alignment with the principles of green chemistry. This reaction effectively addresses various synthetic challenges, especially in the synthesis of natural products. This review carefully examines a selection of articles published from 2014 to 2024, highlighting important optimization conditions and plausible mechanisms.