STUDIES Of NOVEL NITROGEN HETEROCYCLIC COMPOUNDS——SYNTHESIS And ACTIVITY TEST

Nitrogen-containing heterocyclic compounds have a good activity not only in pesticide but also in medicine. They have been researched for a long time. In order to find novel nitrogen heteocyclic pesticide, some compounds were synthesized, their structures were characterized and their biology activities were tested.Part one, twelve compounds were synthesized by "one-pot method", ten of which are firstly reported, the structures of them were confirmed by elemental analysis,IR, MS,and 1H NMR spectrometry. The toxicity of these twelve compounds to Macrophoma kawatsukai was tested with Methyl-Thiophanate as check in laboratory through agar dilution method. The results showed that the compounds have an inhibiting effect on Macrophoma kawatsukai except that two compounds have a growth promotion effect, the EC50 of which is between 4.94~16.14mg/g. The EC95 of five compounds is less than that of Methyl-Thiophanate. Four better active compounds were selected to make fungicide spectrum, using ten pathogenic bacterium which related to many important crops,grains,fruits and vegetables. The EC50 of four compounds to most of pathogenic bacterium is less 30mg/g, the highest value is 80.31mg/g, the least value is 6.92mg/g, which showed these kinds of compounds had some effect on most of pathogenic bacterium and had some broad spectrum quality. Especially, the EC50 of compound (â… b) to all of pathogenic bacterium is about 20mg/g, the EC95 of that is between 50~60mg/g except that the EC95 of that to Venturia inaequalis and Botrytis cinerea are 160.49mg/g and 167.98mg/g.Part two, Three analogue compounds of actamiprid were synthesized by analogue synthesis method through the intermediates which have insecticide activity. The compounds are firstly reported, the structures of which were confirmed by elemental analysis,IR,1H NMR and MS spectrometry.