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A Direct Access to 7‑Aminoindoles via Iridium-Catalyzed Mild C–H Amidation of N‑Pivaloylindoles with Organic Azides

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journal contribution
posted on 29.03.2016, 12:59 authored by Youyoung Kim, Juhyeon Park, Sukbok Chang
Ir­(III)-catalyzed regioselective direct C-7 amidation of indoles in reaction with organic azides has been developed. While its efficiency was varied by the choice of N-directing groups, N-pivaloylindoles were most effective in undergoing the desired amidation at room temperature over a broad range of substrates. The reaction was scalable, and deprotection of the chelation group was also facile.

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