Electrochemical flow aziridination of unactivated alkenes

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