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Design,synthesis and acaricidal activity of novel strobilurin derivatives containing pyrimidine moieties
Authors:Bao‐Shan Chai  Chang‐Ling Liu  Hui‐Chao Li  Xiao‐Min He  Yan‐Mei Luo  Guang Huang  Hong Zhang  Jun‐Biao Chang
Institution:1. State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry, Shenyang, China;2. Department of Chemistry, Zhengzhou University, Zhengzhou, China
Abstract:BACKGROUND: The intermediate derivatisation method based on bioisosteric replacement led to the discovery of the lead strobilurin compound 5a. To produce new strobilurin analogues with improved activity, a series of substituted pyrimidines were synthesised and bioassayed. RESULTS: The compounds were identified by 1H NMR, IR, MS and elemental analysis. The highly active compound 5g was studied by X‐ray diffraction. Preliminary bioassays demonstrated that some of the title compounds exhibited excellent acaricidal activity against Tetranychus cinnabarinus (Boisd.) at 10 mg L?1. The relationship between structure and acaricidal activity is reported. CONCLUSION: The present work demonstrates that strobilurin derivatives containing pyrimidine moieties can be used as possible lead compounds for developing novel acaricides. Copyright © 2010 Society of Chemical Industry
Keywords:strobilurin derivatives  pyrimidine  acaricidal activity  intermediate derivatisation method
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