Endeavor to discover biorational natural products-based insecticides, two series (27) of novel 9-acyloxy derivatives of cinchonidine and cinchonine were prepared and assessed for their insecticidal activity against by the leaf-dipping method at 1 mg/mL. Among all the compounds, especially derivatives and exhibited the best insecticidal activity with final mortality rates of 75.0% and 71.4%, respectively. Overall, a free 9-hydroxyl group is not a prerequisite for insecticidal activity and C9-substitution is well tolerated; the configuration of C8/9 position is important for insecticidal activity, and 9-configuration is optimal; 6'-OCH moiety is not necessary, removal of it is also acceptable. [Formula: see text].
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