摘要
目的证明2,2′脱水衍生物是尿苷类化合物在乙腈(或乙酸乙酯)中与酰卤作用的中间体。方法用改进的方法合成出2,2′脱水尿苷衍生物,与尿苷类化合物和酰卤作用形成的中间体经TLC、熔点、MS、1HNMR等实验进行比较以确认中间体的归属。结果与结论证实了尿苷类酰化卤化过程中的中间体是2,2′脱水尿苷衍生物,这为以2,2′脱水5甲基尿苷为原料合成d4T提供了新的合成途径。
Objective: To prove that 2,2′-anhydrouridine is the intermediate of the reaction of uridine with acyl halide in acetonitrile (or ethyl acetate). Methods: 2,2′-anhydrauride derivative was synthesized using an improved method. Its characters including TLC, mp, MS and 1 HNMR were compared with those of the intermediate of the reaction of uridine with acyl halide, so that the structure of intermediate could be confirmed. Results and Conclusion: Comparison studies prove that the intermediate in acylation and halogention of uridines is 2,2′-anhydrouridine derivative. These results provide a new path to synthesize d4T from 2,2′-anhydro-5-methyluridine.
出处
《药学进展》
CAS
2005年第7期327-331,共5页
Progress in Pharmaceutical Sciences
关键词
尿苷
卤化
酰化
2
2’-脱水尿苷
中间体
Uridine
Acylation
Halogenation
2,2′-Anhydrouridine
Intermediate
