Synthesis And Biological Activity Of A-amino Phosphonates Containing Dipyrimidine Or Uracil

a-Amino phosphonate derivatives as natural amino acid analogues have good insecticidal activity,bactericidal activity and herbicidal activity,and play an increasingly important role in medicinal chemistry and pesticidal science.In order to find the lead compounds with better herbicidal activity,the 4,6-dimethoxypyrimidinyl group was introduced into the a-amino phosphonate sub-structure according to the principle of active substructure splicing.Two types of a-aminophosphonate derivatives ?-5,?-6 and?-6 containing pyrimidine in different forms(22 compounds)are designed and synthesized.In addition,the structure of furan,pyridine,thiophene and benzene were introduced into the sub-structure of a-aminophosphonates,respectively.17 novel a-aminophosphonates were designed and synthesized.Their structures are listed as follows:(1)a-Amino phosphonate compounds containing bis4,6-imethoxypyrimidine and bisphosphono-phosphonate ?-5a??-5f,?-6a??-6c):(2)a-Amino phosphonate compounds containing bis4,6-dimethoxypyrimidine(?-6a??-6m):(3)a-Amino phosphonate compounds containing uracil and other heterocycle(?-10a??-10q):The structures of these compounds have been confirmed by 1H NMR,MS,31P NMR,as well as elemental analyses.The reaction conditions for the synthesis of intermediates and target compounds were optimized.Moreover,the biological activities of the compounds were evaluated.The results showed that parts of the target compounds exhibited good herbicidal activities.