氟达拉宾合成工艺的研究

The Study of 9-β-D-Arabinofuranosyl-2-fluoro-9-H-purin-6-amino Synthesis Process

目的:以2,6-二乙酰氨基嘌呤起始原料合成氟达拉滨。方法:以2,6-二乙酰氨基嘌呤为起始原料,经过成苷、水解、氟取代、脱保护反应制备得到氟达拉滨。结论:产品经过HPLC检测,纯度98.8%。其化学结构通过核磁共振氢谱确证,最终收率为30.8%(以2,6-二乙酰氨基嘌呤计)。该合成工艺路线简单,反应步骤短,反应收率较高,利于实现工业化。

Objective： 2,6-diacetyl aminopurine as starting material,explored the synthesis process of fludarabine. Methods： 2,6-diacetyl aminopurine as the initial raw material, through glycosidation,hydrolysis, fluorine replacing, deprotection reaction 4 steps to prepare fludarabine. Conclusion： The product＇purity was 98.8 % by HPLC detection, and its chemical structure was confirmed by the H-NMR structure, the overall yield was 30.8 %. The process was more simple, less reaction steps, and the reaction yield was higher, which will help to achieve industrialization.