新型含取代异噁唑环的亚硫酸酯类化合物的合成及生物活性研究

为寻求具有较高生物活性的农药新品种,采用活性亚结构拼接法,以醛(1)为原料,经肟化、氯化反应,生成取代氯化肟类化合物(3),化合物3与炔螨特原药经1,3-偶极环加成反应,制得12个未见文献报道的目标化合物(ZJ1~ZJ12)。其结构均经过~1H NMR和MS确证。初步生物活性测定结果表明,在125 mg/L下,化合物ZJ12对朱砂叶螨Tetranychus cinnabarinus的致死率达75%,与炔螨特的杀螨活性相当;在200 mg/L下,化合物ZJ10对测试靶标的根、茎生长抑制率均为100%,优于对照药剂异丙酯草醚。

Synthesis and bioactivities of sulfinic esters containing substituted isoxazolyl moieties

In order to secure novel sulfinic esters with unique biological activities, new compounds were obtained by introducing isoxazole moiety into propargite. Thus, 12 novel compounds(ZJ1-ZJ12)were synthesized by 1,3-dipolar cycloaddition reaction of substituted chlorinated oximes(3) and propargite. Structures of these compounds were confirmed by MS and ¹H NMR. The preliminary bioassay showed that most compounds exhibit good insecticidal and herbicidal activity. The activity of compound ZJ12 against Tetranychus cinnabarinus was as high as propargite. The mortality can reach 75% at a concentration of 125 mg/L. Compound ZJ10 showed 100% inhibitory rates against all the target plants at a concentration of 200 mg/L and the activity of which was better than pyribambenz isopropyl.