Background: Using constantly and widely chemistry insecticides has resulted in a selection
burden and favored tolerance development in various insect species. Particularly, pyrethroids are the
only one which can be used for net impregnation either ITNs or LLIN as yet, however, the excessive
use of pyrethroids has led to many cases of insect resistance in worldwide. Therefore, it is urgent to
develop novel insecticides fighting against this sort of resistance.
Methods: Based on the preliminary studies, we explored a straightforward highly stereoselective
method to achieve the novel chiral ester derivatives by using Oppolzer’s 10,2-camphorsultam as chiral
Results: A series of tetrafluorobenzyl alcohol oriented (S)-enantiomeric esters were designed and synthesized
by the asymmetric synthesis. All the compounds exhibited moderate yields, and the original
synthesized compounds have been evaluated for their potential insecticidal activity against Plutella
xylostella compared with those of fenvalerate and D-trans-phenothrin, and some compounds presented
excellent insecticidal activities.
Conclusion: The bioassay illustrated that some of the compounds exhibit obviously insecticidal activities
against Plutella xylostella, especially, the insecticidal activity of compound 5i was as good as
commercial fenvalerate and D-trans-phenothrin, which can be used as a lead compound for further optimization.