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1,3-Iodo-amination of 2-methyl indoles via Csp2–Csp3 dual functionalization with iodine reagent

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Abstract

A 1,3-iodo-amination with iodine reagent that involved the Csp2–Csp3 dual functionalization of 2-methyl indoles was developed to provide 2-aminomethyl-3-iodo-indole derivatives. The iodo-amination proceeded via a 1,4-transfer of an imide group through the formation of an indolyl(phenyl)iodonium imide using PhI(OAc)2, followed by an iodination using DIH or a double iodination of indole using excess DIH.

Graphical abstract: 1,3-Iodo-amination of 2-methyl indoles via Csp2–Csp3 dual functionalization with iodine reagent

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Publication details

The article was received on 15 Jan 2018, accepted on 09 Feb 2018 and first published on 09 Feb 2018


Article type: Communication
DOI: 10.1039/C8CC00352A
Citation: Chem. Commun., 2018, Advance Article
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    1,3-Iodo-amination of 2-methyl indoles via Csp2–Csp3 dual functionalization with iodine reagent

    K. Moriyama, T. Hamada, K. Ishida and H. Togo, Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8CC00352A

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