Copper-catalyzed Direct Amidation of Heterocycles with N-Fluorobenzenesulfonimide

Pan et al. have reported the copper-catalyzed direct amidation of heterocycles with N-fluorobenzenesulfonimide (NFSI). According to their results, various heteroarenes such as thiophenes, furans, and pyrroles are converted into the α-amidated heterocycle derivatives in high yields by using NFSI as a nitrogen source and CuI as a catalyst. This reaction presumably proceeds via C—H bond activation. It is expected to be used as a novel synthetic method of valuable amidated heterocycles through a direct C—N bond-coupling process.