Study On The Design Synthesis And Biological Activities Of Acyl Ureas And Acyl Thioureas Including Aromatic And Heterocyclic Rings

Near more than 20 in the last years, the acylureas and acyl thioureas have caused the concern of the agrochemical field owing to their insect killing, acaricidal, fungicidal, antivirus, herbicidal and plant growth regulating activities. This kind of compounds have such advantage as high selectivity to non-target living creature, special action mechanism, high surroundings safety, low concentration and quick degradation that traditional agrochemicals can't compare to, was called"the pesticides of 21 centuries".Being the insecticide it inhibits the synthesis of the insect chitin for the purpose of killing the insect, Currently, many new species have been commercialized, becoming the hot spot of the agrochemical research realm- once.By consulting concerned literatures, we reviewed the biological activities, action mechanism and synthetical methods of acylureas and acylthioureas, and the synthetical methods and biological activities of aryloxyacete and substitutedpyrazole, in order to seek insecticides with good biological activities, we have modified the main structure of acylureas and acylthioureas by Bioisosterism Principles and Structure Link Wory , connected aryloxyacete and substitutedpyrazole with the main structure ,and synthesized 21 new acylureas and acylthioureas.Target compounds have been synthesized by condensation of the aromatic nucleus and amino heterocylcle with acyl isocyanates or acylisothiocyanates in absolutely anhydrous and aprotic solvent.Their structures were confirmed by IR,~1H NMR and Elemental analysis. Synthesis condition, spectrum properties and physic-chemical constant of the target compounds were reported at first time. The title compounds are listed as follows.â… . N-(4,6-disubstituted pyrimidine-2-yl)-N'-2,4-dichlorophenoxy acetyl ureas.â…¡. N-(4,6-disubstituted pyrimidine-2-yl)-N'-1-methyl-3-ethyl-4-chloro -5-pyrazolecarboxylic thioureas.