Beyond C2 and C3: Transition-Metal-Catalyzed C–H Functionalization of Indole

Jamie A. Leitch; Yunas Bhonoah; Christopher G. Frost

doi:10.1021/acscatal.7b01785

Beyond C2 and C3: Transition-Metal-Catalyzed C–H Functionalization of Indole

Jamie A. Leitch, Yunas Bhonoah, Christopher G. Frost

Syngenta Ltd

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Abstract

The indole scaffold will continue to play a vital part in the future of drug discovery and agrochemical development. Because of this, the necessity for elegant techniques to enable selective C–H functionalization is vast. Early developments have led to primarily C2 and C3 functionalization because of the inherent reactivity of the pyrrole ring. Despite this, elegant methods have been developed to enable selective C–H functionalization on the benzenoid moiety at C4, C5, C6, and C7. This review focuses on the contributions made in benzenoid C–H functionalization of indoles and other related heteroaromatics such as carbazoles.

Original language	English
Pages (from-to)	5618-5627
Number of pages	9
Journal	ACS Catalysis
Volume	7
Issue number	9
Early online date	11 Jul 2017
DOIs	https://doi.org/10.1021/acscatal.7b01785
Publication status	Published - 1 Sept 2017

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10.1021/acscatal.7b01785

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This document is the Accepted Manuscript version of a Published Work that appeared in final form in Catalysis, copyright (c) American Chemical Society after peer review and technical editing by the publisher. to access the final edited and published work see https://doi.org/10.1021/acscatal.7b01785
Accepted author manuscript, 4.11 MBLicence: Unspecified

Cite this

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AB - The indole scaffold will continue to play a vital part in the future of drug discovery and agrochemical development. Because of this, the necessity for elegant techniques to enable selective C–H functionalization is vast. Early developments have led to primarily C2 and C3 functionalization because of the inherent reactivity of the pyrrole ring. Despite this, elegant methods have been developed to enable selective C–H functionalization on the benzenoid moiety at C4, C5, C6, and C7. This review focuses on the contributions made in benzenoid C–H functionalization of indoles and other related heteroaromatics such as carbazoles.

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Beyond C2 and C3: Transition-Metal-Catalyzed C–H Functionalization of Indole

Abstract

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