Mani Geeta Sai, Donthiboina Kavitha, Shaik Siddiq Pasha, Shankaraiah Nagula, Kamal Ahmed
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad 500037 India
Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology Hyderabad 500007 India
RSC Adv. 2019 Aug 28;9(46):27021-27031. doi: 10.1039/c9ra06005g. eCollection 2019 Aug 23.
A novel strategy towards the synthesis of 1,4-disubstituted 1,2,3-triazoles C-N and N-N bond formation has been demonstrated under transition metal-free and azide-free conditions. These 1,2,3-triazoles were obtained in a regioselective manner from commercially available anilines, aryl alkenes/aryl alkynes and -tosylhydrazines using I under O atmosphere. Broad substrate scope, milder reaction conditions, good to moderate yields and clean protocol are the notable features of the method. Moreover, this protocol is amenable for the generation of a library of medicinally important key building blocks.
在无过渡金属和无叠氮化物的条件下,已经证明了一种合成1,4-二取代1,2,3-三唑(形成C-N和N-N键)的新策略。这些1,2,3-三唑是通过在O气氛下使用I,以区域选择性的方式从市售苯胺、芳基烯烃/芳基炔烃和对甲苯磺酰肼中获得的。底物范围广、反应条件温和、产率良好至中等以及操作简便,是该方法的显著特点。此外,该方案适用于生成一系列具有重要药用价值的关键构建模块。