College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou, Zhejiang, 310058, China.
Org Biomol Chem. 2021 Dec 8;19(47):10376-10384. doi: 10.1039/d1ob01917a.
In the present studies, we describe a convenient and efficient protocol for the synthesis of the indolo[2,1-]isoquinoline core structure through the reaction of 2-aryl--acryloyl indoles and aryl or alkyl α-keto acids under air environment in four hours. The developed approach features broad substrate scope and good functional group tolerance under mild reaction conditions without a metal catalyst participation. A series of valuable indolo[2,1-] isoquinoline derivatives bearing various functional groups were synthesized using this method in good to excellent yields. Based on a series of control experiments, a radical pathway was proposed to explain the experiment.
在目前的研究中，我们描述了一种通过在空气环境中，在四小时内反应 2-芳基--丙烯酰基吲哚和芳基或烷基 α-酮酸，来合成吲哚并[2,1-]异喹啉核心结构的简便、高效的方法。所开发的方法具有广泛的底物范围和良好的官能团耐受性，在温和的反应条件下，无需金属催化剂参与。使用该方法可以以良好到优异的产率合成一系列带有各种官能团的有价值的吲哚并[2,1-]异喹啉衍生物。根据一系列对照实验，提出了一种自由基途径来解释实验。
