Design, synthesis and acaricidal activity of novel strobilurin derivatives containing pyrimidine moieties

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 (1)H NMR, IR, MS and elemental analysis. The highly active compound 5 g 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.