Transition-Metal-Catalyzed Enantioselective Synthesis of Indoles from 2-Alkynylanilines

Abstract Optically active indole derivatives are ubiquitous in natural products and are widely recognized as privileged components in pharmacologically relevant compounds. Therefore, developing catalytic asymmetric approaches for constructing indole derivatives is highly desirable. In this short review, we summarize methods for the transition-metal-catalyzed enantioselective synthesis of indoles from 2-alkynyl­anilines. 1 Introduction 2 Aminometalation-Triggered Asymmetric Cross-Coupling Reactions/Insertion 2.1 Asymmetric Cross-Coupling Reactions 2.2 Asymmetric Insertion of C=O, C=C and C≡N Bonds 3 Asymmetric Relay Catalysis 4 Conclusion