Study On Synthesis And Bioactivity Of Derivatives Of Pyrazolecarboxamides And Thioethers Containing Heterocycles

A great progress has been achieved in recent years in terms of the study of the derivatives of pyrazole and thioether containing heterocycles, which have biological activity and can be used as pesticides, such as, herbicides, fungicides, insecticides, acaricides. The recent studies of them have been reviewed in this thesis.In order to explore novel derivatives of pyrazole and thioether containing heterocycles which have higher biological activity, we designed and synthesized two series of new compounds according to the principle of combination of bioactive substructure and bioisoteric relationship. The structures of the target compounds (Ia-t and Ila-r ) have been confirmed by MS, 1H NMR, IR, Raman spectrum and elemental analysis. And their structures are as follows:During the courses of the synthesis of target compounds Ia-t, we found that when the mixture of chloroform and dimethylsulfoxide(DMSO) was used as solvent, the reactants are in the same phase so that the reaction can happen easily. We also found that when the solvents, such as acetone and methanol which have low boiling points and high polarity, are used in the synthesis of target compounds Ila-r, good yields can be obtained.Primary bioassay showed that some of the compounds have good herbicidal and fungicidal activity. The relationship of structure and bioactivity has been analyzed and discussed primarily.