Synergistic Dual Catalysis in Stereodivergent Synthesis

Chiral skeletons with multiple stereogenic centers widely reside in nature and drugs, and their relative and absolute configuration often determine their physiological or pharmacological properties. Stereodivergent synthesis of chiral molecules is not only of great significance, but also is highly challenging since the formation of one of the diastereomers is inherently preferred in most asymmetric reactions. Stereodivergent dual catalysis, introduced in 2013 by the Carreira group, perfectly catered to all the requirements for full stereoselectivity control of given reactions since two chiral catalysts are utilized in a synergistic way and act independently, and has now been arguably the most efficient strategy to realize stereodivergent synthesis. This comprehensive review presents an overview of the development of stereodivergent synthesis enabled by synergistic dual catalysis in the past ten years, providing readers with the fundamental attributes as well as the ability, scope, mechanism, as well as limitations of this strategy.