2-[4-(对氟苯基)噻唑-2-基]-3-羟基-3-烃氧基丙烯腈的合成及杀菌活性

为了寻找生物活性良好的噻唑基丙烯腈类化合物,利用2-氰甲基-4-(对氟苯基)噻唑( 3 )与取代氯甲酸酯( 4 )在碱存在下反应,合成了15个未见文献报道的2- -3-羟基-3-烃氧基丙烯腈化合物( 5 ),其结构经核磁共振氢谱、质谱和元素分析表征。初步杀菌活性测试结果表明:所有化合物在试验浓度下均具有一定的抑菌活性,尤其对炭疽病菌Colletotrichum gossypii表现出较好的抑制活性,在质量浓度25 mg/L下,所有化合物的抑制率均在50%以上,其中化合物 5a、5e、5g、5k、5n和5o 的抑制率在80%以上。

Synthesis and fungicidal activity of 2-[4-(4-fluorophenyl) thiazol-2-yl]-3-hydroxy-3-hydrocarbyloxy acrylonitriles

In order to find thiazolylacrylonitriles with good biological activity,fifteen novel 2- -3-hydroxy-3-hydrocarbyloxy acrylonitriles 5 were synthesized by reaction of 4-(4-fluorophenyl)-2-thiazoleacetonitrile 3 with substituted chloroformates 4 in the presence of base.The structures of these compounds were confirmed by ¹H NMR,MS spectra and elemental analysis.The preliminary bioassay showed that all compounds exhibited certain fungicidal activity,especially showing good fungicidal activity against Colletotrichum gossypii,the growth inhibition rate of all compounds against Colletotrichum gossypii was above 50%,for compound 5a,5e,5g,5k,5n and 5o were more than 80% at the concentration of 25 mg/L.