N-取代栀子酰胺A衍生物的合成  

Syntheses of N-substituted gardenamide A derivatives

作　　者：杨健[1] 罗军[1] 黄照[1] 陈河如[1] 

机构地区：[1]暨南大学药学院中药及天然药物研究所、广东省中药药效物质基础及创新药物研究重点实验室,广州510632

出　　处：《国际药学研究杂志》2013年第6期790-794,共5页Journal of International Pharmaceutical Research

基　　金：广东省科技计划资助项目(2010A030100006);国家自然科学基金资助项目(81172982)

摘　　要：目的对N-取代栀子酰胺（gardenamide）A的合成方法进行探索。方法以京尼平为起始原料，经选择性保护10位羟基、选择性氧化1位半缩醛、以及与有机胺反应后内酰胺化等过程合成目标化合物。结果通过3步反应合成8个N-取代栀子酰胺A衍生物，3步反应的收率分别为89％、80％和22％-44％。结论3步法合成N-取代栀子酰胺A衍生物步骤简洁，但第3步的反应收率尚有待提高。Objective To investigate the synthesis of N-substituted gardenamide A derivatives. Methods Genipin was used as starting material, and all the target compounds were prepared through the selective protection of 10-hydroxyl group, the selective oxi- dation of 1-semiacetal, and the lactamization when reacted with amines. Results Eight N-gardenamide A derivatives were synthesized via a three-step process. The yields for each steps were 89%, 80% , and 22% -44% respectively. Conclusion Three-step process for the synthesis of N-substituted gardenamide A derivatives is concise. However. the yield for the last step needs to improve.

关 键 词：栀子酰胺A 京尼平 栀子 结构修饰 

分 类 号：R914[医药卫生—药物化学]