Modularity: Adding New Dimensions to Total Synthesis

As the field of synthetic chemistry seeks to tackle new frontiers, total synthesis is primed to address significant medical challenges such as the rise of antibiotic resistance and cancer. One emerging frontier focuses on increasingly concerted efforts to utilize modular total synthesis as a strategy to generate analogs of natural product targets for biological studies, with the ultimate goal of new therapeutic development. This new frontier is enabled by a confluence of human ingenuity in synthetic design, newly developed reactions that facilitate advances in total synthesis strategies, and emerging technologies. In this review, we highlight the evolving trend of modular total synthesis, including new reactions and automated technologies. This trend should lead to an increasingly important source of new medicines to improve human health.