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Issue 18, 2018
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C4–H indole functionalisation: precedent and prospects

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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

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Publication details

The article was received on 16 Dec 2017, accepted on 19 Apr 2018 and first published on 20 Apr 2018


Article type: Perspective
DOI: 10.1039/C7SC05336C
Citation: Chem. Sci., 2018,9, 4203-4216
  • Open access: Creative Commons BY-NC license
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    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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