Issue 18, 2018

C4–H indole functionalisation: precedent and prospects

Abstract

C4-decorated indoles feature in a plethora of bioactive and functional compounds of importance to natural product synthesis, material sciences, as well as crop protection and pharmaceutical industries. Traditionally, their syntheses largely involved harsh stoichiometric metalations and radical reactions. However, transition metal catalysed C–H activation has recently evolved into a powerful strategy for the late-stage diversification of indoles at the C4–H position. Modern photoredox, enzymatic and precious transition metal catalysis represent the key stimuli for developing challenging C–C and C–Het bond forming transformations under mild reaction conditions. Herein, we discuss the evolution and application of these methods for the step-economical transformations of otherwise inert C4–H bonds up to December 2017.

Graphical abstract: C4–H indole functionalisation: precedent and prospects

Article information

Article type
Perspective
Submitted
16 dic. 2017
Accepted
19 abr. 2018
First published
20 abr. 2018
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2018,9, 4203-4216

C4–H indole functionalisation: precedent and prospects

J. Kalepu, P. Gandeepan, L. Ackermann and L. T. Pilarski, Chem. Sci., 2018, 9, 4203 DOI: 10.1039/C7SC05336C

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