Laboratory of Pharmaceutical Design and Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, China.
Bioorg Med Chem Lett. 2012 Sep 1;22(17):5384-7. doi: 10.1016/j.bmcl.2012.07.058. Epub 2012 Jul 21.
In continuation of our program aimed at the discovery and development of natural products-based insecticidal agents, twenty-three new fraxinellone-based hydrazone derivatives were smoothly prepared from fraxinellone via regioselectively allylic oxidation in the presence of selenium dioxide or chromium trioxide under microwave irradiation and subsequent condensation with hydrazides or hydrazines. Their insecticidal activity was evaluated against the pre-third-instar larvae of Mythimna separata Walker in vivo. Especially compounds 6d and 7a displayed the most pronounced insecticidal activity compared with toosendanin, a commercial botanical insecticide derived from Melia azedarach.
在我们旨在发现和开发基于天然产物的杀虫剂的计划的延续中，我们通过二氧化硒或三氧化铬在微波辐射下对 fraxinellone 进行区域选择性烯丙基氧化，然后与酰肼或肼缩合，顺利地从 fraxinellone 制备了 23 种新的 fraxinellone 基腙衍生物。它们对粘虫 Mythimna separata Walker 的预 3 龄幼虫的杀虫活性在体内进行了评估。与从苦楝 Melia azedarach 中提取的商业植物杀虫剂川楝素相比，化合物 6d 和 7a 的杀虫活性最为显著。
