Synthesis And Biological Activities Of Novel Imidazolinones And Thienopyrimidine Derivatives

Many azole compounds have been found to show widespread biological activities. Some of them have been used as fungicide, herbicide, pesticide and medicine .In this paper, we studied the synthesis of novel imidazolones and thienopyrimidines derivatives via aza-Wittig reaction. The spectral properties and biological activities of some compounds were also researched and some of them were found to show good fungicidal activities. More than forty unreported compounds in five parts were synthesized, it may be summarized as follows:1. A new synthetic method to 2-(2-benzothiazolylthio)-3-aryl-5-arylmethylen e-4H-imidazol-4-ones and 2-(2H-1,2,4-triazole)-3-aryl-5,5-dimethyl-4H-imid azol-4-ones was proposed. This synthetic method has the advantage of easily accessible starting material, mild condition and good yields. The reactions of aza-Wittig were studied further.2. We used aza-Wittig reaction to synthesize 2-alkylamino-3-aryI-6-ethyl 5,6-dimethyl-thienopyrimidin-4(3H)-ones and 2-aryIoxy-3-aryl-6-ethyl-5,6-di-methyl -thienopyrimidines-4(3H)-ones. Its mechanism was investigated .3. On the bases of our previous work, The 1-phenyl-2-arylamino-thieno [2,3-d]-1,2,4-triazol[1,5-a]pyrimidin-8(3H)-ones were synthesized under very mild conditions via aza-Wittig reactions.4. The biological activities of partial compounds were studied. The results showed that some of compounds exhibit obviously fungicidal activity. In all these compounds, some exhibited 100% inhibition of Botrytis cinereapers in 50mg/L and a majority of compounds exhibited more than 85% inhibition of Rhizoctonia solani and Botrytis cinereapers, Dothiorella gregaria and Bipolaris maydis in 50mg/L.