Engineering Research Center of Molecular Medicine of Ministry of Education, Key Laboratory of Fujian Molecular Medicine, Key Laboratory of Xiamen Marine and Gene Drugs, School of Biomedical Sciences, Huaqiao University , Xiamen 361021, P. R. China.
Org Lett. 2018 Feb 2;20(3):664-667. doi: 10.1021/acs.orglett.7b03804. Epub 2018 Jan 17.
A highly atom-efficient "one-pot" protocol has been developed to construct multisubstituted 2-hydroxy-benzo[b][1,4]oxazins starting from N-(2-hydroxylaryl)enaminones. This procedure comprises a PIDA-mediated intramolecular iminoenol tautomer trapping reaction, followed by EtN-promoted aerobic oxidative ring construction. In particular, an O molecule from air served as the oxygen source of the hydroxyl group in the titled products. This reaction proceeded smoothly at room temperature under air atmosphere and metal-free conditions.
一种高效原子经济性的“一锅法”策略已被开发出来，用于从 N-(2-羟基芳基)烯胺酮出发构建多取代 2-羟基苯并[1,4]恶嗪。该方法包括 PIDA 介导的分子内亚氨基烯醇互变异构体捕获反应，以及 EtN 促进的有氧氧化环构建。特别地，空气中的一个 O 分子作为标题产物中羟基的氧源。该反应在室温下、空气氛围中和无金属条件下顺利进行。
