Li Guoping, Yan Bing, Wu Liangliang, Li Yabo, Hao Xinqi, Gong Ming, Wu Yangjie
College of Chemistry, Henan Key Laboratory of Chemical Biology and Organic Chemistry, Key Laboratory of Applied Chemistry of Henan Universities, Zhengzhou University, Zhengzhou 450052, China.
Molecules. 2024 Dec 24;30(1):4. doi: 10.3390/molecules30010004.
Isochroman and azole moieties are both present in a wide variety of biologically active molecules. Their efficient combination under mild reaction conditions is beneficial for obtaining small-molecule drug candidates. In this paper, we describe electrochemical α-C(sp)-H/N-H cross-coupling reactions between isochromans and azoles, yielding products in moderate to excellent yields. This protocol does not require any catalysts or exogenous oxidants and can be performed at room temperature under air. Control experiments and cyclic voltammetry showed that the reaction may proceed through both radical coupling and nucleophilic addition processes.
异苯并二氢吡喃和唑类部分都存在于各种各样的生物活性分子中。它们在温和反应条件下的有效结合有利于获得小分子药物候选物。在本文中，我们描述了异苯并二氢吡喃与唑类之间的电化学α-C(sp)-H/N-H交叉偶联反应，产率适中至优异。该方案不需要任何催化剂或外源氧化剂，并且可以在室温下在空气中进行。对照实验和循环伏安法表明，该反应可能通过自由基偶联和亲核加成过程进行。
