Wu Qin, Xu Genrui, Li Weiqiang, Wan Juan, Liu Teng, Huang Chao
National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, School of Chemistry and Environment, Yunnan Minzu University, Kunming 650500, P. R. China.
College of Chemistry and Environmental Science, Qujing Normal University, Qujing 655011, P. R. China.
Org Lett. 2022 Jun 10;24(22):3950-3954. doi: 10.1021/acs.orglett.2c01289. Epub 2022 May 31.
An unprecedented [5 + 2 + 1] cascade cyclization to the preparation of 5-pyrimido[5,4-]indole derivatives has been disclosed. The novel protocol of 2-nitrochalcones reacted with aliphatic primary amines catalyzed by CuI and promoted by CsCO, which underwent a critical intermediate 2,3-disubstituted indole, providing structurally diverse 5-pyrimido[5,4-]indoles in generally high yields (77-90%) and broad substrate scopes (34 examples).
已公开了一种用于制备5-嘧啶并[5,4 - ]吲哚衍生物的前所未有的[5 + 2 + 1]级联环化反应。该新颖的反应方案是2-硝基查尔酮与脂肪族伯胺在碘化亚铜催化和碳酸铯促进下反应，生成关键中间体2,3-二取代吲哚，从而以普遍较高的产率（77 - 90%）和广泛的底物范围（34个实例）提供结构多样的5-嘧啶并[5,4 - ]吲哚。
