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C9-取代
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH · 2021 · IF 1.571

Synthesis of novel 9R/S-acyloxy derivatives of cinchonidine and cinchonine as insecticidal agents

Zhi-Ping Che,Jin-Ming Yang,Song Zhang,Di Sun,Yue-E Tian,Sheng-Ming Liu,Xiao-Min Lin,Jia Jiang,Gen-Qiang Chen

Endeavor to discover biorational natural products-based insecticides, two series (27) of novel 9R/S-acyloxy derivatives of cinchonidine and cinchonine were prepared and assessed for their insecticidal activity against Mythimna separata in vivo by the leaf-dipping method at 1 mg/mL. Among all the compounds, especially derivatives 6l and 6o 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 9S-configuration is optimal; 6’-OCH3 moiety is not necessary, removal of it is also acceptable.

CAS / MDL: 538-75-0 1122-58-3
研究领域: 有机化学 · 植物保护学
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