N-取代栀子酰胺A衍生物的合成

Syntheses of N-substituted gardenamide A derivatives

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.