Direct C–N Coupling of Imidazoles and Benzylic Compounds via Iron-Catalyzed Oxidative Activation of C–H Bonds

A C-H activation protocol used for the benzylation of imidazoles using an Iron catalyst.

This recent paper by Qiu et al. (Hangzhou Normal University, China) can be really interesting for medicinal chemists working with imidazoles and benzimidazoles. To summarize, is a method for the benzylation of the nitrogen without using benzyl halides. The method uses an Iron catalyst, FeCl2, to activate the benzylic C-H bond of diphenylmethanes, methylbenzenes and others. The best yields are obtained with diphenylmethanes. 17 examples are reported with benzimidazoles and 10 with imidazoles, with yields that can be considered good.

J. Org. Chem., Article ASAP. See: 10.1021/jo201253m