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目的:合成4-去乙酰化长春碱氨基酸衍生物,为长春碱靶向前药的合成奠定基础。方法:氨基酸N端采用苄氧羰基(Z)保护,利用混合酸酐法合成(4-去乙酰化长春碱)-氨基酸-Z,然后催化氢化得到(4-去乙酰化长春碱)-氨基酸衍生物。结果:采用新方法合成4-去乙酰化长春碱氨基酸衍生物,结构经质谱和1H-NMR确证。结论:本实验所采用的方法通用性强,优化了反应条件,反应步骤缩短,产率高,产物后处理简便,降低了实验成本。
OBJECTIVE: To synthesize 4-deacetylated vinblastine amino acid derivatives to lay the foundation for the synthesis of vinblastine-targeted prodrugs. Methods: N-terminal amino acid was protected by benzyloxycarbonyl (Z), and (4-deacetylated vinblastine) -amino acid-Z was synthesized by mixed acid anhydride method and then catalyzed by hydrogen to obtain (4- deacetylated vinblastine) . Results: 4-deacetylated vinblastine amino acid derivatives were synthesized by a new method. The structures were confirmed by MS and 1H-NMR. Conclusion: The method used in this study is versatile, optimizing the reaction conditions, shortening the reaction steps, high yield, simple post-treatment and reducing the experimental cost.