新型含吡啶杂环菊酯类化合物的合成及生物活性

Synthesis and Biological Activity of Novel Pyridine-containing Heterocyclic Chrysanthemic Acid Esters

为了寻找新的活性化合物,根据活性亚结构拼接原理,以四丁基溴化铵为相转移催化剂,以3,5-二氯-6取代胺基吡啶杂环的酚钠盐和菊酰氯为原料,在二氯甲烷-水混合体系中合成了一系列新型含吡啶杂环菊酯类化合物。其结构均经1HNMR、13CNMR、IR和MS等分析方法确证。初步生物活性测试结果表明,化合物4e和4f具有有效的杀菌活性,在500mg/L时对黄瓜白粉病菌的抑制率均为100%,对黄瓜炭疽病菌的抑制率分别为60%、56.8%。

In search of novel bioactive compounds,a series of novel pyridine-containing heterocyclic chrysanthemic acid esters were synthesized utilizing sodium 3,5-dichloro-6-substituted amino-pyridin-2-olate and chrysanthemyl chloride as the starting materials in CH2Cl2/H2O system catalyzed by tetrabutyl ammonium bromide. Structures of synthesized compounds were confirmed by 1H NMR,13C NMR,IR and MS. The preliminary bioassay results demonstrated that compounds 4e and 4f exhibited efficient fungicidal activity in vitro. Both of them showed 100% control against sphaerotheca fuliginea,as well as 60% and 56.8% control against colletotrichum lagenarium at 500 mg/L.