New Friedel–Crafts strategy for preparing 3-acylindoles

Abstract

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.