Division of Molecular Synthesis & Drug Discovery, Centre of Bio-Medical Research (CBMR), SGPGIMS Campus, Raebareli Road, Lucknow, 226014, U.P., India.
Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi, 221005, India.
Angew Chem Int Ed Engl. 2021 Apr 12;60(16):8772-8780. doi: 10.1002/anie.202014950. Epub 2021 Mar 5.
An iron-catalyzed denitrogenative rearrangement of 1,2,3,4-tetrazole is developed over the competitive C(sp )-H amination. This catalytic rearrangement reaction follows an unprecedented metalloradical activation mechanism. Employing the developed method, a wide number of complex-N-heterocyclic product classes have been accessed. The synthetic utility of this radical activation method is showcased with the short synthesis of a bioactive molecule. Collectively, this discovery underlines the progress of radical activation strategy that should find wide application in the perspective of medicinal chemistry, drug discovery and natural product synthesis research.
发展了一种铁催化的 1,2,3,4-四唑的脱氮重排反应,该反应在竞争性 C(sp )-H 胺化反应中进行。该催化重排反应遵循一种前所未有的金属自由基激活机制。采用所开发的方法,可以获得大量的复杂含氮杂环产物。该自由基激活方法的合成实用性通过一个生物活性分子的短合成得到了展示。总的来说,这一发现突出了自由基激活策略的进展,该策略应该在药物化学、药物发现和天然产物合成研究方面得到广泛应用。