C6–H Bond Functionalization of Indoles: A New Gate

Abstract

Indoles are valuable precursors in medicinal, bioorganic, and material chemistry and particularly serve as a platform for diversity. However, the scope of the C6-functionalization of indoles was limited until recently. In this short review, we summarize developments in the C6-functionalization reactions of indoles involving transition-metal-catalyzed functionalization and Brønsted and Lewis acid catalyzed processes. The regioselectivity is controlled by remote-C–H activation and hydrogen bond formation.

1 Introduction

2 Transition-Metal-Catalyzed Functionalization

3 Acid-Catalyzed Processes

4 Conclusion

Key words

indole - C–H bond activation - directing group (DG) - transition metal (TM) - acid catalyst - hydrogen bond - electrophilic aromatic substitution (EAS)

Publication History

Received: 03 February 2023

Accepted after revision: 08 March 2023

Accepted Manuscript online:
08 March 2023

Article published online:
12 April 2023

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