Study On Synthesis And Biology Activity Of Substituted Benzimidazoles Derivatives

This thesis includes three chapters.Chapter 1: A brief review for the research of benzimidazole derivaties in recent yearsBenzimidazoles and their derivatives are very useful intermediates for the development of molecules on pharmaceutical or biological interest. Because of their good biological activities and reactive activities, the research of benzimidazoles has been a hot spot. The recent advances in the synthesis and application of benzimidazoles and their derivatives are reviewed in this paper.Chapter 2: Microwave Irradiation-promoted Synthesis and Biology Activity of 2-Aryloxymethylbenzimidazole-1- acetamidesA series of 2-Aryloxymethylbenzimidazole-1-acetamides derivatives were synthesized efficiently and quickly by N-alkylation of 2-aryloxy -methylbenzimidazoles and chloroacetamide derivatives under MWI and PTC conditions using PEG-400 as the phase transfer catalyst. All the products were characterized by elemental analysis, FT-IR, 1H NMR and 13C NMR. The preliminary biological activity tests show that all compounds have the obviously regulating activities for the growth of the wheat.Chapter 3: Study on Synthesis and Biology Activity of Benzimidazole-1-acetylhydrazine DerivativesFirstly, a chievements on the Application of Hydrazine and Related Compounds for the Synthesis of Five-Membered Azole Heterocycles. Secondly, a series of new 5-(2-Aryloxymethylbenzimidazole-1-carbadehyde)-1,3,4 -oxadiazole- 2-thione were synthesized by 2-Aryloxymethylbenzimidazole-1- acetylhydrazines under MWI conditions, The structures of all synthesized compounds were elucidated and confirmed by IR, 1H NMR, 13C NMR and elemental analysis. In the crystal of 6a , the compound was assembled to a linear supramolecular structure along axis b by the intermolecular hydrogen bonds.Crystal data: monoclinic, space group P21/c. The preliminary biological activity tests show that some of the title compounds have obvious regulating activities for the growth of the rape, and some compounds such as 6a and 6h possessed satisfactory activity of growth inhibition against B.subtilis on test concentration. finally, Convenient one-pot synthesis of 5-(2-Aryloxymethylbenzimidazole-1-carbadehyde)-3-ylsulfanyl-4-Amino-1,2,4-triazol from Benzimidazole-1-acetylhydrazine Derivatives.