Recent advances in the reactions of C8-functionalization of substituted tetrahydroquinolines under ruthenium catalyst

Abstract

Scientists are increasingly using ruthenium catalysts to selectively add functional groups to the C8 carbon of tetrahydroquinolines that are versatile class of heterocyclic compounds with diverse applications in chemistry. This article reviews recent advances in ruthenium-catalyzed C8-functionalization reactions of tetrahydroquinolines. We explore different approaches to activate the C8 carbon of tetrahydroquinolines in a controlled way. These approaches include directed ortho-metalation, reactions that use coordination with a metal catalyst, and C-H activation methods. This review showcases the versatility of C8 functionalization, enabling the introduction of a wide range of functional groups including carbon chains (C-C bonds), heteroatoms (C-heteroatom bonds), and even the formation of new rings (cyclization reactions). In this article discusses Ru-catalyzed hydroxylation and acyloxylation reactions of tetrahydroquinolines.Beyond the functionalization itself, the article explores how these C8-modified THQs can be valuable tools for synthesizing complex natural products and potential new drugs. We then deep into the remaining challenges and promising future directions in this area of ruthenium-mediated C8-functionalization, which is experiencing rapid progress.