ABSTRACT

The evolution of molecules on Earth for nearly 3.8 billion years gives us a great opportunity to read incalculable chemical structures with diversity, versatility, and functionality. Over the past centuries, scientists have decoded the valuable chemical genome of our planet through continuously innovated analytical tools.1 In the meanwhile, synthetic chemists dedicated their lifelong careers with never fading passions to natural products’ total synthesis, which was determined as the Mt. Qomolangma (Mt. Everest) of organic synthesis.2 Natural products provide rich sources of information and inspiration; moreover, as gifts of Mother Nature, the natural products library offers us endless possibilities to hunt and create drugs for relieving humans’ pain from disease: Around half of the medicines in stock are derived from natural products.3 As a result, natural products’ total synthesis has drawn attention from not only synthetic and analytical chemists, but also biological, pharmaceutical, and industrial scientists.4 There is no doubt that total synthesis defines and also promotes the frontier of chemistry. Top chemists can now claim that we can conquer molecules with structural complexity in more or less any degree—for example, the distinguished synthesis of longifolene by E. J. Corey,5 esteemed synthesis of palytoxin by Kishi,6 the breathtaking synthesis of brevetoxin B in impressive style by K. C. Nicolaou.7 These are just a glimpse of the milestones in total synthesis history.8