Synthesis And Biological Activity Of α-Amino Phosphonates Containing 4,6-Dimethoxy Pyrimidine

There is a higher requirement for the development of pesticide in new era. High-efficiency, safety and compatibility with the environment will be a basic requirement for green pesticides. Heterocyclic compounds containing pyrimidine has been valued in pesticide industry, due to high biological activity and low toxicity. a-amino-phosphonate and its derivatives are good pesticide candidates and low toxicity and environment benign.Considering heterocyclic compounds containing pyrimidine and a-amino phosphonate and its derivatives have the basic requirements of new pesticides, we try to explore new green pesticides with-a higher biological activity and lower toxicity. In this paper, we designed and synthesized 26 novel a-amino-phosphonate derivatives containing pyrimidine.Their structures of target compound are listed as follows:(1)O,O’-dialky[2-(4,6-dimethoxypyrimidin-2-yloxy)phenyl]-N-(substituted-phenyl)-1-amino-methyl phosphonates 1-2R1=Me、Et、Ph.R2=2-Br、4-F、4-COOEt.(2)O,O’-dialky[2-(4,6-dimethoxypyrimidin-2-sulfanyl)phenyl]-1-amino-1-(substite d-phenyl)-methyl phosphonates Ⅱ-2R1=Me、Et、Ph.R2=H、4-CH3、4-OCH3、4-OH、2-F、4-F、2-C1、3-C1、4-C1、4-Br、3-NO2、 4-NO2、2,4-OCH3、2,4-Cl.The reaction conditions of intermediates and target compounds are discussed indetail. In addition all target compounds have been confirmed by 1H NMR,31P NMR, MS, IR techniques and elemental analysis. The preliminary biological activity of the title compounds were evaluated.