阿德福韦酯的合成工艺优化及质量控制  

Synthetic process optimization and quality control of Adefovir dipivoxil

作　　者：沈广志[1] 郭强[1] 于凤波[1] 梁启超[1] 吴宜艳[1] 邹桂华[1] SHEN Guangzhi;GUO Qiang;YU Fengbo;LIANG Qichao;WU Yiyan;ZOU Guihua(School of Pharmaceutical Sciences,Mudanjiang Medical University,Mudanjiang 157011,China)

机构地区：[1]牡丹江医学院药学院,黑龙江牡丹江157011

出　　处：《实验室科学》2021年第2期34-36,共3页Laboratory Science

基　　金：黑龙江省省属高等学校基本科研业务费科研项目(项目编号:2018-KYYWFMY-0012)。

摘　　要：阿德福韦酯是开环膦酸核苷酐类抗病毒药物,是阿德福韦的酯类前体药物,具有广谱的抗病毒活性。阿德福韦酯合成工艺中的酯化反应,质量不稳定,收率较低。在现有合成工艺路线文献报道的基础上,通过对反应温度、反应时间、投料比等因素的研究,重新优化合成工艺,并进行质量控制。采用正交设计法,重点考察反应温度(A)、投料比(B)、反应时间(C)3个因素对阿德福韦酯酯化反应的影响。通过实验研究,确定了阿德福韦酯酯化反应的最佳工艺条件为A2B1C1,提高了产品质量和收率。Adefovir dipivoxil is an acyclic nucleoside phosphonates antiviral agents,it is the ester prodrug adefovir,with broad-spectrum antiviral activity.However,because of the low yield and unstable of the last step reaction the ester.In this paper,based on the synthetic technologies reported in the literature,optimization of reaction temperature,reaction time and material ratio and other key items.The new orthogonal experimental design is used,emphasizing on three factors including the reaction temperature(A),the weighter ratio of material(B)and reaction time(C)on the yield.The best reaction condition is A2B1C1.The results showed that the product yield and quality was improved by optimizing the conditions.

关 键 词：抗病毒药 阿德福韦酯 合成 

分 类 号：R914[医药卫生—药物化学]