盐酸吉西他滨合成工艺改进

目的：提高盐酸吉西他滨合成收率。方法：通过对盐酸吉西他滨合成中的关键反应——胞苷形成反应条件的改进,进而提高胞苷形成反应的选择性,从而使产品收率提高。结果：对盐酸吉西他滨合成中的关键反应——胞苷的形成反应进行了优化,提高选择性,进而提高产品收率。结论：以苯甲醚为溶剂,氯化锂和硫酸钾为催化剂,在120～125℃下,反应选择性达到1/9,3β收率最高可达到81.2%。

Improvement of synthetic process of gemcitabine hydrochloride

Objective: To improve the synthetic yield of gemcitabine hydrochloride. Methods: Through improving the form condition of cytidine,which was the key reaction of forming gemcitabine hydrochloride,the selectivity of cytidine reaction was improved,and then yield was increased. Results: The improvement for the selectivity of cytidine reaction made the yield of the product increase. Conclusion: Using anisole as a solvent and using lithium chloride and potassium sulfate as catalysts,under the temperature of 120 ～ 125℃,the reaction selectivity may achieve 1/9,and the yield of 3β may increase to 81.2% at most.