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The discovery of SYP‐10913 and SYP‐11277: novel strobilurin acaricides
Authors:Bao‐Shan Chai  Chang‐Ling Liu  Hui‐Chao Li  Hong Zhang  Shao‐Wu Liu  Guang Huang  Jun‐Biao Chang
Affiliation:1. State Key Laboratory of the Discovery and Development of Novel Pesticides, Shenyang Research Institute of the Chemical Industry, Shenyang, China;2. Department of Chemistry, Zhengzhou University, Zhengzhou, China
Abstract:BACKGROUND: As previously reported, methyl (E)‐2‐[2‐(2‐phenylamino‐6‐trifluoromethylpyrimidin‐4‐yloxymethyl)phenyl]‐3‐methoxyacrylate has proven to be a new lead with highly acaricidal activity. Following on from this, in an effort to discover new strobilurin analogues with improved activity, a series of substituted pyrimidines were synthesised and bioassayed. RESULTS: All compounds were characterised by 1H NMR, IR, MS and elemental analysis. Preliminary bioassays demonstrated that some of the title compounds exhibited notable control of Tetranychus cinnabarinus (Boisd.) at 1.25 mg L?1. The relationship between structure and acaricidal activity is discussed. CONCLUSION: Two compounds of particular interest, 6j (SYP‐10913) and 6k (SYP‐11277), exhibited potent acaricidal activity. The acaricidal potencies of these analogues are higher than that of fluacrypyrim in greenhouse applications, and are comparable with those of commercial acaricides such as spirodiclofen and propargite in field trials. Copyright © 2011 Society of Chemical Industry
Keywords:strobilurin  pyrimidine  acaricidal activity  intermediate derivatisation method
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