College of Chemistry & Chemical Engineering, Yibin University, Yibin, Sichuan, China.
Org Biomol Chem. 2021 Feb 7;19(5):998-1003. doi: 10.1039/d0ob02286a. Epub 2021 Jan 15.
An efficient and practical electrochemically catalyzed transition metal-free process for the synthesis of substituted quinazolinones from simple and readily available o-aminobenzonitriles and aldehydes in water has been accomplished. I/base and water play an unprecedented and vital role in the reaction. By electrochemically catalysed hydrolysis of o-aminobenzonitriles, the synthesis of quinazolinones with benzaldehyde was first proposed. The synthetic utility of this method was demonstrated by gram-scale operation, as well as the preparation of bioactive N-(2,5-dichlorophenyl)-6-(2,2,2-trifluoroethoxy) pteridin-4-amine, which enables straightforward, practical and environmentally benign quinazolinone formation.
已实现一种高效实用的电化学催化过渡金属自由方法，可从简单易得的邻氨基苯甲腈和醛在水中合成取代的喹唑啉酮。I/base 和水在反应中发挥了前所未有的重要作用。通过电化学催化水解邻氨基苯甲腈，首次提出了以苯甲醛合成喹唑啉酮的方法。该方法的合成实用性通过克级操作以及生物活性 N-(2,5-二氯苯基)-6-(2,2,2-三氟乙氧基)蝶啶-4-胺的制备得到了证明，这使得喹唑啉酮的形成变得直接、实用且环境友好。
