Angew. Chem. Int. Ed. 2017, 56, ASAP.
Direct functionalization of natural products is important for studying structure-activity and structure-property relationships of these molecules. Recent advances in transition-metal-catalyzed functionalizations of C(sp3 )-H bonds, the most abundant yet inert bonds in natural products, have been shown to create natural product derivatives selectively. Strategies to achieve such transformation are reviewed.