Zi Quanxing, Li Minyan, Cong Jielun, Deng Guogang, Duan Shengzu, Yin Meng, Chen Wen, Jing Hong, Yang Xiaodong, Walsh Patrick J
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education; Yunnan Provincial Center for Research & Development of Natural Products; School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P. R. China.
Roy and Diana Vagelos Laboratories, Penn/Merck Laboratory for High-Throughput Experimentation, Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104, United States.
Org Lett. 2022 Mar 11;24(9):1786-1790. doi: 10.1021/acs.orglett.2c00140. Epub 2022 Feb 25.
Herein is introduced the application of "super-electron-donor"(SED) 2-azaallyl anions in a tandem reduction/radical cyclization/radical coupling/aromatization protocol that enables the rapid construction of isoquinolines. The value of this transition-metal-free method is highlighted by the wide range of isoquinoline ethyl amines prepared with good functional group tolerance and yields. An operationally simple gram scale synthesis is also conducted, confirming the scalability.
本文介绍了“超电子给体”（SED）2-氮杂烯丙基阴离子在串联还原/自由基环化/自由基偶联/芳构化反应中的应用，该反应能够快速构建异喹啉。这种无过渡金属方法的价值体现在制备的一系列异喹啉乙胺具有广泛的官能团耐受性和良好的产率。还进行了操作简单的克级合成，证实了其可扩展性。
