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

Organic & Biomolecular Chemistry Pub Date: 2022-03-01 DOI: 10.1039/D1OB02383G

Abstract

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.

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