含1,3,4-噻二唑杂环的甲氧基丙烯酸酯类化合物的合成与杀菌活性研究有机化学.pdfVIP

DOI: 10.6023/cjoc201306032 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 含1,3,4-噻二唑杂环的甲氧基丙烯酸酯类化合物的合成与 杀菌活性研究 袁小勇a,b 张 鹭a 韩小强a 周子原a 杜士杰a 万 川a 杨冬燕a 覃兆海*,a (a 中国农业大学理学院 北京 100193) (b 赣州师范高等专科学校 赣州 341000) 摘要 以多种取代苯甲酸为原料, 通过酰化、醇解、肼解、亲核加成、脱水、亲核取代等多步反应, 合成了 16 个未见 文献报道的含 1,3,4-噻二唑杂环的甲氧基丙烯酸酯类化合物, 其结构均通过 1H NMR, IR, MS, HRMS 等予以表征确认, 并对所有化合物进行了离体杀菌活性测试. 结果表明: 对水稻立枯和棉花枯萎病菌的防效好于番茄晚疫病菌, 对西瓜 炭疽病菌防效显著, 其中化合物 5a～5c, 5g, 6a～6c 的抑制率均高于嘧菌酯, 5g 在 100 μg/mL 下抑制率为 77.5%. 关键词 1,3,4- 噻二唑; 甲氧基丙烯酸酯; 合成; 杀菌活性 Synthesis and Fungicidal Activity of the Strobilurins Containing 1,3,4-Thiodiazole Ring Yuan, Xiaoyonga,b Zhang, Lua Han, Xiaoqianga Zhou, Ziyuana Du, Shijiea Wan, Chuana Yang, Dongyana Qin, Zhaohai*,a (a College of Science, China Agricultural University, Beijing 100193) (b Ganzhou Teachers College, Ganzhou 341000) Abstract Sixteen novel strobilurins containing 1,3,4-thiodiazole ring were synthesized by multi-step reactions including acylation, alcoholysis, hydrazinolysis, nucleophilic addition, dehydration and nucleophilic substitution from initial substituted benzoic acid and their structures were characterized by 1H NMR, IR, MS and HRMS. The results of bioassay indicated that the fungicidal activity of title compounds is better against Rhizoctonia s