自印楝素被分离鉴定以来,其广谱而独特的生物活性受到人们的广泛关注,已成为一种近乎完美的植物源杀虫剂;且在医药、保健、日化等领域都有广泛的应用.其复杂而独特的分子结构使得科研工作者进行了大量的全合成尝试、结构修饰及构效关系等研究.综述了印楝素A的片段合成、全合成和印楝素有关的结构修饰以及生物活性等方面的研究进展. Since the separation and identification of azadirachtin, its broad-spectrum and unique biological activity has drawn people’s attention and has become a near-perfect plant-derived insecticide. It has a wide range of applications in medicine, healthcare, Application.The complex and unique molecular structure enables researchers to do a lot of research on total synthesis, structure modification and structure-activity relationship.It is summarized that the fragment synthesis of azadirachtin A, the total synthesis and the structural modification of azadirachtin As well as biological activity and other aspects of research progress.