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    An efficient approach to access functionalized indole derivatives has been developed through Cu(OTf)2-catalyzed C3 aza-Friedel-Crafts alkylation of substituted indoles 5a-5m, N-methyl-pyrrole with linear N,O-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.


    Zi-Juan Yi, Jian-Ting Sun, Tian-Yu Yang, Xian-Yong Yu, Xiao-Li Han, Bang-Guo Wei. Cu(OTf)2-catalyzed C3 aza-Friedel-Crafts alkylation of indoles with N,O-acetals. Organic & biomolecular chemistry. 2022 Mar 16;20(11):2261-2270

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    PMID: 35229848

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