Design, Synthesis, and Structure-Activity Relationship of Novel Spiropyrimidinamines as Fungicides against .

J Agric Food Chem

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.

Published: June 2020

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.

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http://dx.doi.org/10.1021/acs.jafc.9b07055DOI Listing

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