多杀菌素B的半合成制备方法

Semisynthesis of spinosyn B

摘要: 多杀菌素B具有很好的杀虫活性,但其天然含量很低,不易获得。作者以单质碘、乙酸钠和氢氧化钠为反应试剂,甲醇为溶剂,通过对反应条件优化,成功地将多杀菌素A中福乐糖胺氮原子上的1个甲基脱去,建立了一条以来源丰富的多杀菌素A为原料,简便、高效合成多杀菌素B的方法,多杀菌素B收率高达81%,为其开发应用及衍生研究奠定了基础。多杀菌素B的结构经1H NMR、13C NMR和HRESI-MS表征。

Abstract: Spinosyn B bears very potent insecticidal acitivity. However, it is difficult to obtain because of its low concentration in natural. In this paper, spinosyn B was successfully synthesized from spinosyn A, the major component in spinosad, utilizing iodine, sodium acetate and sodium hydroxide as reagents and methanol as the solvent. After optimization, the yield has been improved to 81%. The structure of spinosyn B was confirmed by 1H NMR, 13C NMR and HRESI-MS.