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Cu(OTf) 2 -catalyzed C3 aza-Friedel-Crafts alkylation of indoles with N , O -acetals

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...

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Published in:Organic & biomolecular chemistry 2022-03, Vol.20 (11), p.2261-2270
Main Authors: Yi, Zi-Juan, Sun, Jian-Ting, Yang, Tian-Yu, Yu, Xian-Yong, Han, Xiao-Li, Wei, Bang-Guo
Format: Article
Language:English
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Summary: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/d1ob02383g