Wacker Oxidation: A Powerful Tool for Natural Product Synthesis

Abstract Wacker oxidation is an aerobic oxidation of olefins that has emerged as an active area of research in terms of natural product synthesis as well as access to nonnatural and drug candidates. The synthesis of complex molecules by terminal oxidation of functionalized olefins via Markovnikov and anti‐Markovnikov fashion has enabled the total synthesis of numerous natural products. The efficiency, functional group tolerance, and uniqueness of the Wacker protocol have attracted chemists in designing novel strategies for complex bioactive scaffolds. This article provides an overview of the application of Wacker oxidation in the synthesis of bioactive alkaloids and oxygen‐containing heterocycles. Besides this, significant attempts toward construction of highly challenging natural products via Aza ‐Wacker oxidation are also described. A special emphasis is placed on compiling new breakthroughs in synthetic methods to achieve complex bioactive frameworks during the period 2011–2024.