Syntheses of N-substituted gardenamide a derivatives / 国际药学研究杂志

ABSTRACT

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 he selective protection of 10-hydroxyl group, the selective oxidation of 1 -semiacetal, and he lactamization when reacted with amines. Results Eight A'-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.