التفاصيل البيبلوغرافية
| العنوان: |
Electrochemical flow aziridination of unactivated alkenes. |
| المؤلفون: |
(王盛淳), Shengchun Wang, (王鹏杰), Pengjie Wang, (李树劲), Shu-Jin Li, (陈宜鸿), Yi-Hung Chen, (孙志军), Zhi-Jun Sun, (雷爱文), Aiwen Lei |
| المصدر: |
National Science Review; Oct2023, Vol. 10 Issue 10, p1-10, 10p |
| مصطلحات موضوعية: |
DRUG discovery, METAL catalysts, MITOMYCIN C, ALKENES, AZIRIDINES, AZIRIDINATION, AMINATION, MITOMYCINS |
| مستخلص: |
Aziridines derived from bioactive molecules may have unique pharmacological activities, making them useful in pharmacology (e.g. mitomycin C). Furthermore, the substitution of the epoxide moiety in epothilone B with aziridine, an analog 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 report 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 undergo simultaneous oxidation or alkene is oxidized preferentially. Further anticancer treatments in cell lines have demonstrated the pharmacological activities of these aziridines, supporting the potential of this method for drug discovery. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
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