A series of novel 1,2,4-triazole derivatives were synthesized from o-fluorobenzoic acid, hydrazine hydrate, phenyl isothiocyanate by multi-step reactions. Their structures were characterized by 1 H NMR, MS and elemental analyses. The target compounds were evaluated for their fungicidal activities against Corynespora cassiicola, Pseudomonas syringae pv. Lachrymans, Pseudoperonospora cubensis and Sclerotinia sclerotiorum in vivo, and the results indicated that some of the title compounds displayed excellent fungicidal activities.

To find new pesticidal lead compounds with high bioactivity, 18 acylthioureas contain 1,3,4-thiadizols were obtained by condensation between acyl isothiocyanate and 1,3,4-thiadiazols. Their structures were confirmed by 1 H NMR and MS. The herbicidal activities of these compounds were evaluated. All the compounds have herbicidal activity at 200 g ai/ha. The bioassay results showed that compound 5b had 90% inhibitory effect against Echinochloa crusgalli, Setaira viridis, Digitaria sanguinalis, Amaranthus retroflexus and Eclipta prostrate at 200 g ai/ha in pre-emergence condition and 90% and 95% against Echinochloa crusgalli and Eclipta prostrate at 200 g ai/ha in post-emergence condition, respectively; and compound 5e had 100% inhibitory effect against Echinochloa crusgalli, Setaira viridis, Digitaria sanguinalis and Amaranthus retroflexus at 200 g ai/ha in post-emergence and post-emergence condition.

李倩梅 a 庞凯胜 a 赵建平 b 刘幸海 a 翁建全 * ,a ( a 浙江工业大学化学工程学院 杭州 310032)

In order to find novel biologically active pesticide lead compounds, twenty-one novel 3-[(5-benzylthio-1,3,4-oxadiazol-2-yl)methyl]benzo[d]thiazol(oxazol)-2(3H)-ones were synthesized by 2-benzothiazolinone/benzoxazolone as starting materials via substitution, hydrazine, cyclization and the last benzylation reaction. The structures of the title compounds were characterized by 1 H NMR, IR, EI-MS and elemental analysis. The preliminary bioassay results indicated that most of them showed moderate inhibition activity against Colletotrichum orbiculare, Botrytis cinerea and Rhizoctonia solani at 50 mg/L, and the inhibition rate of compound 5b against Botrytis cinerea and Rhizoctonia solani reached above 85%.

化合物对黄瓜(Cucumis sativus)、 小麦(Triticum aestivum)、 高粱(Sorghum vulgare)、 萝卜(Raphanus sativus)、 油菜(Brassica campestris)和稗草(Echinochloa crusgalli)的根和茎的抑制率在 85%以上.