节点文献
磷酸氟达拉滨的制备
Preparation of Fludarabine Phosphate
【摘要】 以氟达拉滨为原料，与磷酸三乙酯和三氯氧磷反应制得磷酸氟达拉滨，所得产品收率约81%，纯度99.91%。该工艺反应条件温和、操作简便且工艺稳定，已完成工艺验证，适合工业化生产。
【Abstract】 An improved synthetic process of fludarabine phosphate(1) was developed. Commercially available fludarabine was subjected to a nucleophilic substitution with triethyl phosphate. Subsequently, the target compound 1 was obtained through hydrolysis of triethyl phosphate on exposure to phosphorus oxychloride condition with an overall yield of 81% and a purity of 99.91%. The optimized process bearing mild reaction conditions, simple operation and stable process had been tested by process verification, and was suitable for industrial production.
【关键词】 磷酸氟达拉滨；
磷酸三乙酯；
三氯氧磷；
合成；
【Key words】 udarabine phosphate； triethyl phosphate； phosphorus oxychloride； synthesis；
【Key words】 udarabine phosphate； triethyl phosphate； phosphorus oxychloride； synthesis；
【基金】 国家自然科学基金项目(21602045);河南省高等学校重点科研项目计划(21A150002);河南师范大学研究生科研创新项目(YL202110)
- 【文献出处】 中国医药工业杂志 ,Chinese Journal of Pharmaceuticals , 编辑部邮箱 ,2024年08期
- 【分类号】TQ463;R914
- 【下载频次】1