Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Org Lett. 2013 Feb 15;15(4):844-7. doi: 10.1021/ol303533z. Epub 2013 Jan 31.
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.
我们实现了铜催化的唑类分子内和分子间烷氧基化反应。该反应是过渡金属催化杂环芳烃 C-H 烷氧基化的罕见实例。此外，烷氧基化反应甚至在克级规模下也能很好地进行。在大多数分子间烷氧基化反应中，需要使用过量的醇（在某些情况下，醇可用作溶剂）才能有效地促进烷氧基化反应，但这种烷氧基化反应仅使用 1 当量的醇即可进行。
