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Mol Divers. 2013 Nov;17(4):641-9. doi: 10.1007/s11030-013-9460-z. Epub 2013 Jul 19.

Palladium-catalyzed regioselective synthesis of 2(2'-biphenyl)benzimidazoles through C-H activation.

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  • 1Laboratory of Combinatorial Drug Design, Department of Applied Chemistry, National Chiao Tung University, Hsin-chu, 300-10, Taiwan.


An efficient palladium-catalyzed strategy through C-H bond activation for the synthesis of 2(2[Formula: see text]-biphenyl)-benzimidazoles is reported herein. The regioselective C-C bond formation proceeds in a sealed tube via oxidative C-H activation of ortho-directed 2-aryl-benzimidazole to couple with various iodobenzene analogs in high yields. This arylation exhibited high regioselectivity which is able to increase molecular diversity in difficult functionalized positions of parent molecules. This strategy provides a convenient and simple synthesis of biphenyl heterocyclic compounds with high regioselectivity.

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