α-萘乙酰硫脲和酰胺衍生物的合成及其抑制作物病菌活性

Syntheses and Antifungal Activities of α-Napthaleneacetic Acid Derivatives

以高活性的α-萘乙酸为前体,通过相转移催化剂,得到萘乙酰异硫氰酸酯,再分别与含吡啶环、吡唑环、萘环、含氟苯环等活性基团的胺反应,合成了3个酰基硫脲衍生物和3个酰胺类化合物,其中3a、3b、3d、3e、3f为新化合物。经IR、MS、1H NMR和元素分析确认了化合物的结构。同时对2种植物病原菌进行了初步的生物活性测试。结果表明,在50 mg/L时,所有化合物对棉花枯萎病菌和棉花红腐病菌都有较好的抑菌活性,其中对棉花红腐病菌的抑制率均在70%以上。

With α-napthaleneacetic acid as precursor, three thiourea derivatives and three carboxamides derivatives were synthesized by solid-liquid phase transfer catalytic reaction. Compounds 3a, 3b, 3d, 3e, 3f are new compounds. The structures were confirmed by means of IR, ^1H NMR, MS and elemental analysis. The results of biological test show that all of these compounds have good antifungicidal activities. The antifungal activities to Fusarium moniliforme could reach 70% when their centrations is around 50 mg/L