基于Ugi反应的新型鱼尼丁受体杀虫剂的设计、合成及生物活性

利用Ugi 反应设计合成了一系列未见文献报道的α-苯基-α-酰胺基-酰胺类化合物, 所有化合物均通过 ¹H NMR谱、元素分析和高分辨质谱表征确定. 初步的生物活性测试结果表明, 在浓度为200 mg/L时, 化合物7h对粘虫有一定抑制活性; 在浓度为50 mg/L时, 化合物7q对苹果轮纹病菌、化合物7e对小麦赤霉菌有一定的抑菌活性.

Design, Synthesis and Biological Activities of New Ryanodine Receptor Pesticides Based on Ugi Reaction

Chlorantraniliprole,invented by DuPont company in 2001,is a new type of insecticide with high efficiency,low toxicity,broad-spectrum insecticidal activity which act at Ryanodine receptor of target insects.Both flubendiamide and chlorantraniliprole contain two amide groups in different locations of the structure,and this could be of great significance in insecticidal activity.Referring to their structural composition,a series of novel α-phenyl-α-amide-amide compounds was designed and synthesized.We changed chlorantraniliprole’s β-amino-acid-amide to the α-phenyl-α-amide-amide.The Ugi reaction was carried on to uphold diversity in the molecular.A series of compounds was obtained and bio-assayed and their structure-activity relationship was discussed.Also,their structures were characterized by 1H NMR,elemental analysis and HRMS.The preliminary results of biological activity experiment show that the compounds at 200 mg/L exhibit some insecticidal activity against Mythimna separate(7h);the compounds also exhibit some fungicidal activity against Physalospora piricola(7q) and Alternaria solani(7e).