Synthesis And Properties Of Herbicidal Of Benzene Sulfonyl Triazole-Pyrimidine Derivatives And Their Interaction With Calf Thymus DNA

Pyrimidine derivatives and triazole derivatives are widely existed in natural products,drug molecules,and show a wide range of useful biological,pharmacological properties such as pesticides,fungicides,herbicides,anti-metabolism,anti-tumor.In recent years,the synthesis and biological activity of these derivatives has become one of hot topics in the current biological and pharmacological study.In an attempt to discover novel heterocyclic compounds with high herbicidal activity,eighty novel triazole-pyrimidine compounds were designed and synthesized by incorporating the activated structural templets of triazole and pyrimidine in this paper.Their structures were confirmed by IR,¹H NMR,¹³C NMR,¹⁹F NMR,HRMS and X-ray single crystal diffraction.A preliminary bioassay of these title compounds was studied.This paper is mainly divided into the following three parts:1.Eighty unreported benzene sulfonyl triazole-pyrimidine derivatives of three series were synthesized and their structures were confirmed.?:5-{1-phenylsulfonyl-5-[?phenoxy?methyl]-1H-1,2,4-triazol-5-yl}-2-alkylthio-6-?methylthio?pyrimidin-4-amine?41??:5-{1-phenylsulfonyl-5-[?fluorophenoxy?methyl]-1H-1,2,4-triazol-5-yl}-2-alkylthio-6-?methylthio?pyrimidin-4-amine?18??:5-{1-[?fluorophenyl?sulfonyl]-5-phenoxymethyl-1H-1,2,4-triazol-5-yl}-2-alkylthio-6-?methylthio?pyrimidin-4-amine?21?2.All newly synthesized compounds were screened for herbicidal activities against monocotyledonous and dicotyledonous plants.The results indicated that many target compounds possessed good herbicidal activity.The structure-activity relationship was researched.Some title compounds with excellent herbicidal activity were also screened for IC₅₀ against cucumber.3.The way some target compounds interacted with calf thymus DNA was studied.