Many natural products have intriguing biological properties that arise from their fascinating chemical structures. Numerous synthetic methods/strategies have been invented to improve the efficiency of natural-product synthesis. A broad group of compounds with diverse functionalities for various applications (e.g., development of new drugs) are available. However, the intrinsic complexity of the structural skeleton and the reactive functional groups on natural products pose tremendous challenges to chemical syntheses. Hypervalent(III) iodine has demonstrated its synthetic versatility by enabling various transformations (e.g., skeletal rearrangement, cyclization and/or cycloaddition and sp3 C–H bond functionalization), which have been utilized widely in the synthesis of natural products. Here, recent innovations of hypervalent(III) iodine in natural-product synthesis are described and discussed.
