阿维菌素B_(2a)大环内酰胺的合成及生物活性

Synthesis and Biological Activity of Avermectin B_(2a) Macrolactam

以阿维菌素B_(2a)为原料,经保护、开环、氧化、胺化和关环5个步骤合成目标化合物阿维菌素B2a大环内酰胺。通过核磁共振氢谱(1 HNMR)、基质辅助激光解吸电离飞行时间质谱(MALDI-TOF-MS)、高分辨质谱(HRMS)等对目标化合物进行结构表征,并测定了目标化合物对东方粘虫、棉铃虫、蚊幼虫及朱砂叶螨的杀虫活性。结果表明,在浓度为10mg·L^(-1)时,目标化合物对幼螨的杀虫活性高达70%,优于阿维菌素B2a。

Using avermectin B_（2a） as a raw material,we synthesized the target compound avermectin B（2a） macrolactam through five steps of protection,ring-opening,oxidation,amination,and ring-closing.We characterized the structure of the target compound by 1 HNMR,MALDI-TOF-MS,and HRMS.Furthermore,we determinated the insecticidal activities of the target compound against Mythimna separate Walker,Helicoverpa armigera,Culex pipiens,and Tetranychus cinnabarinus.The results show that the insecticidal activity of the target compound against larva is up to 70% at the concentration of 10 mg·L^（-1）,which is superior to that of avermectin B_（2a）.