2-Aminobenzimidazoles are widely presenti na number of bioactive molecules. Generally,t he preparation of these molecules could be realized by the mono-substitution of 2-halobenzimidazoles with amines. However,r are examples were reported for the di-substituted products and the selectivity of mono-v s. di-substitution wasr elatively low. Considering the potentialv alues of the di-substituted products, we accomplished the first selective diheteroarylationo f amines with 2-halobenzimidazoles. Notably,this Pd-catalyzed transformationw as realized under ligand-free conditions. Accordingly, numeroust arget productsw ere efficiently produced from various aromatic or aliphatic amines and 2-halobenzimidazoles. It was worth notingt hat two representative products were further confirmed by X-ray crystallography. More significantly,t his catalytic process could be applied to the synthesis and discoveryo fn ew bioactive compounds, which demonstrated the synthetic usefulness of this newly developeda pproach.[a] W. Sang, Dr.Y .Y uan,D r. C. Chen,P rof. Dr.F .V erpoort
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