关键词: 合成, 膦酸盐, 除草活性, 杀菌活性

For the purpose of studying the structure-activity relationship of O-alkyl α-(substituted phenoxyacetoxy)alkylphosphonic derivatives, fourteen novel O-alkyl α-(substituted phenoxyacetoxy)alkylphosphonates were synthesized by the reactions of key intermediate 3 with NaI or LiBr. The intermediate 3 was prepared by the treatment of α-hydroxyalkylphosphonates 1 with substituted phenoxyacetyl chlorides 2 which could be easily obtained by the reaction of substituted phenoxyacetic acids with excess thionyl chloride. The structures of compounds 4 have been confirmed by ¹H NMR, IR, MS and elemental analyses. The results of preliminary bioassay indicated that most of title compounds possess significant herbicidal and fungicidal activities. Compound 4a showed 100% inhibitory activity against all the tested species in the rate of 1.5 kg/ha. Compounds 4h～4m exhibited more than 90% inhibitory activity against Sclerotinia sclerotiorum and Botrytis cinerea in the rate of 50 μg/g.

Key words: synthesis, phosphonate, herbicidal activity, fungicidal activity