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Issue 1, 2013
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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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The article was received on 06 Aug 2012, accepted on 05 Sep 2012 and first published on 06 Sep 2012

Article type: Perspective
DOI: 10.1039/C2SC21185H
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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