Total Synthesis

Abstract

Total synthesis is the production of a molecule from commercially or readily available chemicals through a series of chemical reactions including bio‐mediated transformations. In the first quarter of the twenty‐first century, most complex molecules are, in principle, accesible through total synthesis. However, often, complex molecules can only be prepared in small amounts of a few milligrams. Therefore, the challenges of total synthesis in the XXIth century is the efficiency by which required amounts of a product can be prepared in the shorter time possible. In this article, different types of syntheses are discussed. These are divided into four classes: target‐oriented synthesis (TOS), combinatorial synthesis (CS), diversity‐oriented synthesis (DOS), and diverted total synthesis (DTS). The concepts, challenges, and requirements of each class are introduced and relevant examples, from classic to contemporary, including Woodward's synthesis of strychnine, are discussed.