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Indole synthesis – something old, something new

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Indoles, both naturally occurring and synthetic, exhibit wide-ranging biological activity. Unusual and complex molecular architectures occur among their natural derivatives. As a result, this important ring system continues to attract attention from the international chemical community, and new methodologies for the construction of this ever relevant heteroaromatic ring continue to be developed. Unfortunately, many methods frequently start from ortho-substituted anilines, thereby greatly restricting the availability of starting materials. A more general approach would start from a mono-functionalized arene such as an aniline or halobenzene, followed by cyclization with C–C or C–N bond formation to an unactivated C–H bond. Such methods are the subject of this perspective.

Graphical abstract: Indole synthesis – something old, something new

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Article information

06 Aug 2012
05 Sep 2012
First published
06 Sep 2012

Chem. Sci., 2013,4, 29-41
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Indole synthesis – something old, something new

M. Inman and C. J. Moody, Chem. Sci., 2013, 4, 29
DOI: 10.1039/C2SC21185H

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