龚智华, 胡莎, 金学平, 余磊, 朱园园*, 古双喜*    

DOI: 10.7536/PC211207      

录用日期: 2022-04-01

摘要: 磷酸酯类前药与原药相比，不仅能够提高药物靶向性、稳定性和生物利用度，减少药物毒副作用，还能掩蔽药物不适气味、提高水溶性从而改善给药途径。含有羟基药物的磷酸酯化是该类药物前药设计的重要方法之一。本文对不同磷酸化试剂进行分类，综述了磷酸酯类前药的合成方法与应用，并展望了其发展趋势。

Abstract  Compared with the original drugs, the phosphoester prodrugs can not only improve the targeting, stability and bioavailability of the drugs, reduce toxicity and side effects, but also mask the unpleasant odor of the drugs, improve water solubility, and provide better access to the drugs. Phosphorylation of hydroxyl-containing drugs is one of the important methods for their prodrug design. In this review, we summarize the preparation methods of phosphoesters as prodrugs according to different phosphorylation reagents, and prospect their development trends.

引用：

龚智华, 胡莎, 金学平, 余磊, 朱园园, 古双喜. 磷酸酯类前药的合成方法与应用[J]. 化学进展 , 2022, DOI: 10.7536/PC211207.

Zhihua Gong, Sha Hu, Xueping Jin, Lei Yu, Yuanyuan Zhu, Shuangxi Gu. Synthetic Methods and Application of Phosphoester Prodrugs[J]. Progress in Chemistry , 2022, DOI: 10.7536/PC211207.