丙烯腈类化合物的合成及除草活性

Synthesis and Herbicidal Activities of Acrylonitrile Compounds

[目的]设计合成一系列丙烯腈类化合物并测试其除草活性。[方法]以取代乙腈为原料,经酰化反应制得α-羰基乙腈类中间体,分别与不同的胺发生缩合反应生成席夫碱,并经过互变异构生成14个目标化合物。[结果]化合物结构经~1H NMR和MS确证。初步活性测试结果表明：在200 mg/L质量浓度下,目标化合物均具有较好的除草活性。其中,化合物ZJ1、ZJ7和ZJ8对高粱和油菜根茎的抑制率均超过90%。[结论]化合物的除草活性优于对照药剂异丙酯草醚。

[Aims] The purpose is to design and synthesize novel acrylonitrile derivatives and to evaluate its herbicidal activities. [Methods] α-Carbonyl acetonitrile were synthesized using substituted acetonitriles as the raw materials by acylation reactions. Then fourteen novel title compounds were synthesized by condensation reaction of substituted amines with α-carbonyl acetonitrile intermediates. [Results] The structure ofthe compounds were confirmed by ~H NMR and MS. The preliminary bioassay showed that the target compounds exhibited good herbicidal activities at the concentration of 200 mg/L. For example, compounds ZJ1, ZJ7 and ZJ8 displayed over 90% inhibition against stems and roots of sorghum and rape. [Conclusions] The herbicidal activities of the target compounds were better than that of pyribambenz isopropyl.