College of Chemistry, Sichuan University, Wangjiang Road 29, Chengdu, Sichuan 610064, China.
National Anti-Drug Laboratory Sichuan Regional Center, 36 Yunling Road, Chengdu, Sichuan 610200, P.R. China.
J Org Chem. 2023 Jul 7;88(13):9518-9522. doi: 10.1021/acs.joc.3c00609. Epub 2023 Jun 1.
A straightforward strategy for direct benzylic C-H bond amination an electrochemical Ritter-type reaction is developed. The reaction demonstrates simpler and milder reaction conditions over the existing methods without extra mediator. Moderate to excellent yields up to 94% of the desired amide products were obtained with a broad substrate scope. The removal of the Ac group by a simple step can afford NH-free benzylic amines, providing a suitable approach for the late-stage functionalization of bioactive molecules.
开发了一种直接苄基 C-H 键胺化的直接策略——一种电化学 Ritter 型反应。与现有方法相比，该反应在无需额外介体的情况下具有更简单、更温和的反应条件。具有广泛底物范围的所需酰胺产物的产率达到中等至优异，高达 94%。通过简单的一步去除 Ac 基团可以得到无 NH 的苄基胺，为生物活性分子的后期官能化提供了一种合适的方法。
