新型(3R,3aR,6aS)六氢呋喃并[2,3-b]呋喃烟碱类化合物的合成及活性研究

Synthesis and Activity of (3R,3aS,6aR)-Hexahydrofuro[2,3-b]furan-neonicotinoid Compounds

以(3R,3aS,6aR)六氢呋喃并[2,3-b]呋喃-3-醇(8)为原料通过酯化反应、SN_2亲核取代反应、Pd/C催化还原以及缩合反应制备一系列新型的(3R,3aS,6aR)六氢呋喃并[2,3-b]呋喃烟碱类化合物。对路线中酯化试剂的选择、亲核反应的溶剂、温度和反应时间进行了优化;并且对化合物以蚕豆蚜为靶标进行了活性测试,其中化合物4的活性较好,浓度为1.0×10^(-5)mg/L时死亡率为65.96%。

（3R,3aS,6aR）-Hexahydrofuro[2,3-bl turan neonlcouno, of reactions including esterification of （3R,3aS,6aR）-hexahydrofuro [2,3-b] furan-3-ol, SN2 nucleophilic substitution, reduction using palladium on carbon as catalyst and condensation reaction. The choice of esterification reagents and soNeut, temperature, time of nucleophilic reaction were optimized in detail in this paper. And the activity tests of resulting compounds on target bean aphid were carried out, and results indicated compound 4 was of the best activity with a mortality rate of 65.96% at a loading of 10 mg/L.