Design, Synthesis, and Structure–Activity Relationship of New Pyrimidinamine Derivatives Containing an Aryloxy Pyridine Moiety Aiying Guan Changling Liu Wei Chen Fan Yang Yong Xie Jinbo Zhang Zhinian Li Mingan Wang 10.1021/acs.jafc.6b05580.s001 https://acs.figshare.com/articles/journal_contribution/Design_Synthesis_and_Structure_Activity_Relationship_of_New_Pyrimidinamine_Derivatives_Containing_an_Aryloxy_Pyridine_Moiety/4622290 The pyrimidinamine diflumetorim is an ideal template for the discovery of agrochemical lead compounds due to its unique mode of action, novel chemical structure, and lack of reported resistance. To develop a new pyrimidinamine fungicide effective against cucumber downy mildew (CDM), a series of new pyrimidinamine derivatives containing an aryloxy pyridine moiety were designed and synthesized by employing the recently reported intermediate derivatization method (IDM). The structures of all compounds were identified by <sup>1</sup>H NMR, elemental analyses, HRMS, and X-ray diffraction. Bioassays demonstrated that some of the title compounds exhibited excellent fungicidal activities against CDM. Compound <b>9</b> gave the best activity (EC<sub>50</sub> = 0.19 mg/L), which is significantly better than the commercial fungicides diflumetorim, flumorph, and cyazofamid. The relationship between structure and fungicidal activity of the synthesized pyrimidinamines was explored. The study showed that compound <b>9</b> is a promising fungicide candidate for further development. 2017-01-25 00:00:00 compound 9 fungicide candidate fungicides diflumetorim title compounds pyrimidinamine diflumetorim X-ray diffraction aryloxy pyridine moiety 1 H NMR fungicidal activities Compound 9 IDM New Pyrimidinamine Derivatives Containing EC 50 fungicidal activity derivatization method pyrimidinamine derivatives novel chemical structure CDM Aryloxy Pyridine Moiety pyrimidinamine fungicide cucumber downy mildew HRMS