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 sp 3 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. The focus article discusses the innovation of hypervalent( iii ) iodine regarding skeletal rearrangement, cycloaddition and cyclization, and sp 3 C-H functionalization in natural product synthesis.