Suzuki-Miyaura coupling under microwave enhanced conditions: synthesis of 2-(hetero)aryl benzimidazoles

An expedient, palladium-mediated cross-coupling approach to functionalize the benzimidazole-based core under microwave-assisted conditions has been developed and is described. This protocol, which incorporates appendage diversity on this potential scaffold, is found to be compatible with a wide range of electronically and sterically-divergent (hetero)aryl boronic acids. The use of the PdCl2/(SPhos) catalytic system allows the formation of a stable and highly active LPd(0) species which was found to be critical for the successful synthesis of these novel, pharmacologically-relevant molecules. [GRAPHICS] .