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磷酸氟达拉滨的制备

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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,己完成工艺验证,适合工业化生产.
Preparation of Fludarabine Phosphate
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.

fludarabine phosphatetriethyl phosphatephosphorus oxychloridesynthesis

郝二军、赵琰、贾茹萍、宋禹漫、崔杨波、李桐、卢丙辉

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河南师范大学化学化工学院,精细化学品绿色制造河南省协同创新中心,绿色化学介质与反应教育部重点实验室,河南新乡 453007

磷酸氟达拉滨 磷酸三乙酯 三氯氧磷 合成

国家自然科学基金项目河南省高等学校重点科研项目计划河南师范大学研究生科研创新项目

2160204521A150002YL202110

2024

中国医药工业杂志
上海医药工业研究院,中国化学制药工业协会

中国医药工业杂志

CSTPCD
影响因子:0.487
ISSN:1001-8255
年,卷(期):2024.55(8)