Key Laboratory of Theoretical Organic Chemistry Functional Molecule, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, People's Republic of China.
Department of Natural Medicine, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
Org Biomol Chem. 2022 Mar 16;20(11):2261-2270. doi: 10.1039/d1ob02383g.
An efficient approach to access functionalized indole derivatives has been developed through Cu(OTf)-catalyzed C3 aza-Friedel-Crafts alkylation of substituted indoles 5a-5m, -methyl-pyrrole with linear ,-acetals 4a-4l. As a result, a series of C3 amide aza-alkylated indole derivatives 6a-6ag and 7 were synthesized in moderate to excellent yields.
一种高效的方法已经被开发出来，可以通过 Cu(OTf)催化的取代吲哚 5a-5m、-甲基吡咯与线性 -，-缩醛 4a-4l 的 C3 氮杂-Friedel-Crafts 烷基化反应来获得功能化的吲哚衍生物。结果，一系列 C3 酰胺氮杂烷基化的吲哚衍生物 6a-6ag 和 7 以中等至优异的产率合成。
