Shengchun Wang (王盛淳), Pengjie Wang (王鹏杰), Shu-Jin Li (李树劲), Yi-Hung Chen (陈宜鸿), Zhi-Jun Sun (孙志军), Aiwen Lei (雷爱文).National Science Review.（雷爱文、孙志军、陈宜鸿）

Abstract：

        The Aziridines derived from bioactive molecules may have unique pharmacological activities, making them used in pharmacology (e.g. mitomycin C). Furthermore, the substitution of the epoxide moiety in epothilone B with aziridine, an analogue of epoxides, yielded a pronounced enhancement in its anticancer efficacy. Thus, there is interest in developing novel synthetic technologies to produce aziridines from bioactive molecules. However, known methods usually require metal catalysts, stoichiometric oxidants, and/or pre-functionalized amination reagents, causing difficulty in application. A practical approach without a metal catalyst and extra-oxidant for the aziridination of bioactive molecules is in demand, yet challenging. Herein, we reported an electro-oxidative flow protocol that accomplishes an oxidant-free aziridination of natural products. This process is achieved by an oxidative sulfonamide/alkene cross-coupling, in which sulfonamide and alkene are simultaneous oxidation or alkene is oxidized preferentially. Further anticancer treatments in cell lines demonstrated these aziridines' pharmacological activities, supporting the potential of this method for drug discovery.      

        论文链接：https://doi.org/10.1093/nsr/nwad187