Copper-catalyzed C-H alkoxylation of azoles.

Org Lett

Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

Published: February 2013

We achieved copper-catalyzed intramolecular and intermolecular alkoxylation of azoles. This reaction is a rare example of transition-metal-catalyzed C-H alkoxylation of heteroaromatic compounds. In addition, the alkoxylation reaction proceeded well even in gram scale. In most intermolecular alkoxylations, the use of an excess amount of alcohols (in some cases, alcohols are used as a solvent) is indispensable to efficiently promote the alkoxylation reaction, but this alkoxylation reaction proceeded using only 1 equiv of alcohols.

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Source
http://dx.doi.org/10.1021/ol303533zDOI Listing

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