Synthesis and Herbicidal Activity of α‐Hydroxy Phosphonate Derivatives Containing Pyrimidine Moiety

Abstract

AbstractA series of α‐hydroxy phosphonate derivatives containing pyrimidine moiety were designed and synthesized. Their structures were characterized by IR, 1H NMR, MS and elemental analysis. The results of preliminary herbicidal activities (in vitro) showed that some of the title compounds 2 exhibited moderate herbicidal activities against dicotyledonous weeds (Brassica campestris L), and most of compounds 2 showed better activity against dicotyledonous weeds than monocotyledonous weeds (Echinochloa crus‐galli). Further bioassays (in vivo) indicated that some of the title compounds 2 possessed good and selective herbicidal activity against amaranth pigweed (A. retroflexus) in both pre‐ and post‐emergence treatments at the dose of 1.5 kg/ha. For exmple, compounds 2a, 2b and 2e exhibited 100% inhibition against A. retroflexus in pre‐emergence treatment, and 91.7%, 98.8% and 99.5% inhibition in post‐emergence treatment at the dose of 1.5 kg/ha, respectively.