Synthesis And Biologically Active Study Of 2-aryloxymethylbenzimidazole Derivatives

This thesis includes three chapters.Chapter1: Study of the synthesis of 2-aryloxymethylbenzimidazole derivatives.In this section, the former research work on synthesis and application of benzimidazole, which were to say, are discussed, and a series 2-aryloxymethylbenzimidazole were synthesized under microwave irradiation condition. Compared with classic methods, it has the advantages of quick, high-yield, clean and work-up easy. The ratio of moles of raw materials is n(o-phenylendiamine): n(2-aryloxyacetic acids) =1∶1.1. The best ratio of volume of catalyst is V(PPA)∶V(HCl)= 1∶1. The available power of microwave irradiation is 650～850W .The reaction time is 10～15minutes.The structures of all the compounds were conformed by elemental analysis, IR, ¹H NMR, ¹³C NMR and MS.Chapter 2: Synthesis of 2,2 - arydioxymethyldibenzimidazoleIn this section, Three compounds of 2,2 -arydioxymethyldibenzimidazole were Synthesized under microwave-irradiation using polyphosphoric acid and 4M hydrochloric acid(PPA-HCl ) as Catalyst. o(m-,p-)phenylenedioxydiacetic and o-phenylendiamine as started materials. The available power of microwave irradiation is 650～850W. The reaction time is 10～15minutes.Their structures were confirmed by IR, ¹HNMR, ¹³CNMR, MS and elementary analysis . this procedure has the advantages of sample operaration ,short reaction times.Chapter3: Study of the Synthesis and bioactivity of 2-aryloxymethylbenzimidazole- 1-acetic acidsIn this section,. A series of 2-aryloxymethylbenzimidazole-1-acetic acids were synthesized under microwave irradiation and phase transfer catalysis conditions in good yields. The structures of all the compounds were conformed by elemental analysis, IR, ¹H NMR and ¹³C NMR. the bioactivity of the compounds were investigated.In summary, we synthesized 2-aryloxymethylbenzimidazoles, arydioxymethyldibenzimidazolyle and 2-aryloxymethylbenzimidazole -1-acetic acids in this thesis. By the optimization of the reaction conditions, we give good methods of synthesizing these three kinds of compounds, which are attractive for their advantages shown in the thesis.