通过吲哚衍生物的叠氮化反应实现电氧化C-N键形成：通往3-取代-2-(唑-1-基)吲哚的途径。
Electro-Oxidative C-N Bond Formation through Azolation of Indole Derivatives: An Access to 3-Substituent-2-(Azol-1-yl)indoles.
作者信息
Zhou Naifu, Zhao Junhao, Sun Chengbo, Lai Yuqin, Ruan Zhixiong, Feng Pengju
机构信息
Department of Chemistry and Guangdong Provincial Key Laboratory of Functional Supramolecular Coordination Materials and Applications, Jinan University, Guangzhou 510632, China.
Key Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Science, and the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China.
出版信息
J Org Chem. 2021 Nov 19;86(22):16059-16067. doi: 10.1021/acs.joc.1c01271. Epub 2021 Sep 14.
A practical protocol to synthesize 3-substituent-2-(azol-1-yl)indole derivatives has been developed via an electrochemical oxidative cross coupling process under mild conditions. This electro-oxidative C-N bond formation strategy tolerates a range of functional groups and is amenable to gram scale synthesis. Moreover, this method was applied to the late-stage functionalization of bioactive molecules.
一种通过电化学氧化交叉偶联过程在温和条件下合成3-取代-2-(唑-1-基)吲哚衍生物的实用方案已被开发出来。这种电氧化C-N键形成策略能够耐受多种官能团，并且适用于克级规模的合成。此外，该方法还应用于生物活性分子的后期官能团化。
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