Studies On Synthesis And Biological Activity Of Phosphonate,Amide And Fused Heterocyclic Derivatives Containing Pyridine And Thiazole

The heterocyclic compounds containing nitrogen atom such as triazole, pyridine and thiazole rings, possess a broad spectrum of biological activity. They play a key role in modern chemical pesticides. In order to find novel lead heterocyclic compounds containing nitrogen, we designed and synthesized three series of novel heterocyclic compounds containing of pyridine and thiazole rings. Totally, 47 new novel tatget including 11 new intermediates compounds were obtained. Their structures were characterized by ~1H NMR and elemental analysis, some of them were characterized by EI-MS, IR and X-ray crystal diffraction analysis. The general formulas of these compounds are listed as follows:The reactions of ethyl N-3-((6-chloropyridin-3-yl)methyl)-5-substituted-3H-1,2,3-triazol-4-ylformimidate with various of N-H compounds were studied, different products were observed.In this paper, different reaction conditions and their properties of physical, chemical and spectroscopy of these title compounds were systematically investigated.The results of preliminary bioassay showed the triazolo-[4,5-d]pyrimidine compounds and amide compounds containing pyridine and thiazole display moderate insecticidal and fungicidal activities. Phosphonate compounds containing pyridine and thiazole displayed some extent of fungicidal and herbicidal activities. In addition, the structure-activity relationships of the target compounds were discussed.