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A novel and efficient chemoenzymatic selective formation C-N bond method in the synthesis of 2-substituted benzimidazole heterocycle catalyzed by lipase from porcine pancreas (PPL) has been developed.A series of 2-substituted benzimidazole derivatives were synthesized under mild conditions with high yields (89-96%) and high selectivity.The optimal ethanol solvents, 10 mg enzyme amount and 35 ℃ temperature were screened.