Novel Substituted Anilinopyrimidine Compounds: Design, Synthesis, And Fungicidal Activity

DISCOVERY AND SYNTHESIS OF CROP PROTECTION PRODUCTS(2014)

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摘要
Anilinopyrimidinones exhibited moderate fungicidal activity against cucumber downy mildew (CDM) or wheat powdery mildew (WPM) in previous research. To improve their bioactivity, a series of novel anilinopyrimidine analogs were designed and synthesized using 'Intermediate Derivatization Method'. Preliminary bioassays demonstrated that most of the compounds exhibited weak to moderate activities against downy mildew. But surprisingly, some compounds synthesized showed moderate to good fungicidal activities against powdery mildew. The relationship between structure and fungicidal activity was also discussed. Compounds 7a-4 exhibited potent fungicidal activity against powdery mildew and effective in the control of powdery mildew on wheat, strawberry, tomato, cucumbers at 250-300 mg/L in field trials.
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