Principles for Synthetic Efficiency and Expansion of the Field

Today, the field of natural product total synthesis, which was once a dominant sub‐discipline of organic chemistry, has lost its prime position. Even with the renaissance of natural products as drug candidates, and the recent recognition of the value and contribution of natural product‐based drugs to societies by the Nobel Prize in Physiology or Medicine 2015, the situation has changed. As we have mentioned in the Introduction, “it is estimated that half of the top 100 best‐selling medications will soon be biologics.” According to Dirk Trauner, “the field is currently under fire, at least in societies that have traditionally supported it.” To address these challenges, we need to significantly improve efficiency of the synthesis, expand the field of total synthesis, and address the concerns of society. In this chapter, the efforts by chemists from these dimensions will be summarized with a focus on concepts.