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Hepatitis B virus (HBV)-associated liver diseases are now one of the serious health problems in the world. In this paper, HBV and its biological characteristics are described briefly, and the development of anti-HBV agents is discussed in detail. We focus largely on the design and synthesis of the l-methyl-1H-benzo[d]imidazol-5-ol derivatives.Based on the former research work, we found that 5-hydroxy-1H-indole derivatives has good anti-HBV activity. Taking Arbidol as lead compound, the indole ring is taken place by benzimidazole ring with the bioisosterism and a series of novel benzimidazole derivatives are designed. Taking 4-nitrophenol as starting materials, through 9 to 13 steps of benzyl -protecting, reduction, acylation, nitration, reduction-cyclization, desprotecting, Mannich reaction, monoxidation and dioxidation, totally 30 target compounds never reported in literatures are synthesized, and their structures are confirmed by MS and ~1H-NMR. Their anti-HBV activities are under investigation.
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