Efficiency, Diversity, and Complexity with Multicomponent Reactions

Abstract Multicomponent reactions (MCRs) are versatile syntheses for obtaining structurally diverse sets of complex scaffolds with high efficiency. As such, they can be attractive synthetic tools for the realization of diversity- and/or biology-oriented synthesis design strategies for focused libraries. In this account, we present an overview of our contribution to the design of novel MCRs to access a high level of molecular complexity and diversity. In addition, we demonstrate our biocatalysis/MCR sequences to obtain stereoenriched product scaffolds. 1 Introduction 2 The Build/Couple/Pair Strategy 3 Rational Design of Multicomponent Reactions 3.1 Single Reactant Replacement 3.2 Modular Reaction Sequences 3.3 Conditions-Based Divergence 3.4 The Combination of Multicomponent Reactions 4 Palladium-Catalyzed Isocyanide Reactions 5 The Quest for Stereoselective Multicomponent Reactions 6 Conclusion