Oxazosulfyl类似物的合成及杀虫活性测定

Synthesis and determination of insecticidal activity of oxazosulfyl analogues

为发现具有较高杀虫活性的先导化合物,设计并合成了一系列含硫醚(亚砜、砜)的Oxazosulfyl类似物,并测试了其杀虫活性。以邻氨基苯硫酚(Ⅰ)为起始原料,经6步反应得到15个目标化合物。反应总收率为20.2%~37.1%,产物纯度为95%~97%。其结构经1H NMR、EMI-MS确证。杀虫活性测定结果表明:化合物A_(1)、C_(1)、D_(3)、E_(2)对小菜蛾和粘虫均具有良好的杀虫活性,可作为先导化合物进行进一步的化合物设计、合成等研究。

In order to explore the lead compounds with high insecticidal activity,a series of oxazosulfyl analogues containing sulfone and sulfoxide were designed and synthesized,and their insecticidal activities were tested.The 15 target compounds were synthesized via six steps with 2-aminobenzenethiol as strating material.The total yield of the products were 20.2%~37.1%and the purity was 95%~97%.The structures were confirmed by 1H NMR and EMI-MS.The results showed that some compounds had insecticidal activity against Plutella xylostella and Mythimna seperata,such as:A_(1)、C_(1)、D_(3)、E_(2).It can be used as lead compounds for further study of compounds design and synthesis.