Many natural products have remarkable biological functions due to their fascinating molecular architectures. Despite many advances in synthetic method development, the efficient synthesis of highly functionalized and structurally intricate natural products to meet the demand for biological investigations remains a daunting challenge. Molecular editing encompassing insertion, deletion, or exchange of atoms of highly functionalized compounds has emerged as a hotspot in new method development and has been applied in complex natural product synthesis. In this highlight, the latest developments in molecular editing in natural product synthesis are discussed.