Electrochemically promoted annulation of aldehydes and carbazates: access to 2-alkoxy/aryloxy-5-substituted 1,3,4-oxadiazole and 1,3,4-oxadiazol-2(3<i>H</i>)-one derivatives
作者:Hongjun Li、Dong Tang、Zafar Iqbal、Yaya Wan、Rui Jiang、Zhixiang Yang、Jinhui Yang
DOI:10.1039/d2nj04113h
日期:——
The strategy is oxidant-free and transition-metal free, offering the electrolyte-free completion of the reaction at room temperature. A possible mechanism has been proposed based on control-experiment results and literature reports. The practical utility of this approach is highlighted via the brief synthesis of 5-(4-chloro-3-(trifluoromethyl)phenyl)-1,3,4-oxadiazol-2(3H)-one, which is a potent inhibitor
通过醛的环化,开发了一种高效且环保的化学和药学上有趣的 2-烷氧基/芳氧基-1,3,4-恶二唑和 1,3,4-恶二唑-2(3 H )-酮的合成方法和卡巴酸盐。该协议涉及以电化学方式促进以良好至优异的产量获得所需产品。该方法使用 NaBr 作为电催化剂,MeOH 作为溶剂。该策略不含氧化剂和过渡金属,可在室温下无电解质完成反应。基于对照实验结果和文献报道提出了一种可能的机制。通过5-(4-chloro-3-(trifluoromethyl)phenyl)-1,3,4-oxadiazol-2( 3 H)-one,它是 Notum 羧酸酯酶活性的有效抑制剂。