4.6 Article

New Friedel-Crafts strategy for preparing 3-acylindoles

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 16, Issue 42, Pages 7792-7796

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8ob02094a

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Funding

  1. National Natural Science Foundation of China [NSF21472073, NSF21532001, NSF21772075]

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A selective Friedel-Crafts acylation of indoles via an unusual cleavage of the amide C-N bond was achieved by triflic anhydride activation. This method offers rapid efficient access to high-biological-value 3-acylindoles, performs a series of scrupulous mechanistic studies and offers a strong courage that amide synthons can form new C-C bonds under transition-metal-free conditions.

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