为了寻找具有生物活性的新化合物,以氟乙酸甲酯、氰乙酰胺和甲酸乙酯为起始原料,经环合、氯化、水解、酰氯化等反应合成了一系列含氟吡啶杂环酰胺类化合物,其结构均经,HNMR、^13C NMR、IR和MS确证。初步生物活性测试结果表明,部分化合物对菌虫表现出一定的活性。化合物2f对孑孓(Culex pipiens)在50mg/L时有100%的死亡率,在250mg/L时对黄瓜白粉病菌(Sphaerotheca fuliginea)也有21%的抑制活性.
In search of novel bioactive compounds, a series of fluorine-containing pyridine-heterocyclic acylamide compounds were synthesized starting from the materials of methyl fluoroacetate, cyanacetamide and ethyl formic ester via ring closure, chlorination, hydrolyzation and acylchloriration reaction. All novel compounds were confirmed by ^1H NMR, ^13C NMR, IR and MS. The preliminary bioassay results showed that some compounds exhibited certain antifungal and insecticidal activities. Compound 2f exhibited 100% mortality against Culex pipiens at 50 mg/L and showed 21% inhibition against Sphaerothecafuliginea at 250 mg/L.