The endeavor of total synthesis and its impact on chemistry, biology and medicine

The synthesis of urea in 1828 set in motion the discipline of organic synthesis in general and of total synthesis in particular, the art and science of synthesizing natural products, the molecules of living nature.Early endeavors in total synthesis had as their main objective the proof of structure of the target molecule.Later on, the primary goal became the demonstration of the power of synthesis to construct complex molecules through appropriately devised strategies, making the endeavor an achievement whose value was measured by its elegance and eiciency. While these objectives continue to be important, contemporary endeavors in total synthesis are increasingly focused on practical aspects, including method development,eiciency, and biological and medical relevance. In this article, the emergence and evolution of total synthesis to its present state is traced, selected total syntheses from the author’s laboratories are highlighted,and projections for the future of the ield are discussed.