State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R&D Co. Ltd., Shenyang 110021, People's Republic of China.
J Agric Food Chem. 2020 Jun 17;68(24):6485-6492. doi: 10.1021/acs.jafc.9b07055. Epub 2020 Jun 4.
Harmful fungus and the developed resistance to available fungicides seriously threaten the yield and quality of crops; thus, the search for new, highly efficient, and resistance-overcoming fungicides remains a quite urgent goal of agricultural scientists. In this study, a series of novel spiropyrimidinamine derivatives were designed and synthesized by employing the intermediate derivatization method (IDM). Their structures were identified by H NMR, elemental analyses, and MS spectra. The structure of compound was further confirmed by X-ray diffraction. Bioassays indicated that a number of the title compounds exhibited some fungicidal activities against . Especially, compound displayed excellent activity (EC = 0.422 mg/L), significantly higher than those of the commercialized fungicides cyazofamid, flumorph, and diflumetorim. The structure-activity relationship was also discussed. It was concluded that compound with super fungicidal potency and a novel structure is a promising agrochemical fungicide candidate for further development.
有害真菌和对现有杀真菌剂的抗性严重威胁着作物的产量和质量；因此，寻找新的、高效的、克服抗性的杀真菌剂仍然是农业科学家的一个非常紧迫的目标。在这项研究中，采用中间体衍生化方法（IDM）设计和合成了一系列新型螺吡喃胺衍生物。通过 1H NMR、元素分析和 MS 谱确定了它们的结构。通过 X 射线衍射进一步证实了化合物 的结构。生物测定表明，一些标题化合物对 表现出一定的杀菌活性。特别是化合物 表现出优异的活性（EC = 0.422 mg/L），显著高于商品化杀真菌剂氰霜唑、氟吗啉和氟吡菌胺。还讨论了构效关系。结论是，化合物 具有超强的杀菌活性和新颖的结构，是一种有前途的农用杀菌剂候选物，值得进一步开发。
