Abstract

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.

摘要

努力发现基于生物理性天然产物的杀虫剂，制备了两类（27）新的辛可尼定和辛可宁的9 R / S-酰氧基衍生物，并通过叶浸法以1 mg的剂量评估了它们对体内Mythimna separata的杀虫活性。/毫升 在所有化合物中，尤其是衍生物6l和6o表现出最好的杀虫活性，最终死亡率分别为75.0％和71.4％。总的来说，游离的9-羟基不是杀虫活性的先决条件，并且C9取代具有良好的耐受性。C8 / 9位的构型对于杀虫活性是重要的，而9 S构型是最佳的。6'-OCH ₃ 部分不是必需的，也可以将其除去。