| 替诺福韦的合成工艺改进 |
| |
| 引用本文： | 刘嘉,李科,孙海玲,冯继禄.替诺福韦的合成工艺改进[J].药学实践杂志,2009,27(1):31-32,45. |
| |
| 作者姓名： | 刘嘉 李科 孙海玲 冯继禄 |
| |
| 作者单位： | 第二军医大学药学院药物化学教研室,上海,200433 |
| |
| 摘 要： | 目的：改进替诺福韦的合成工艺。方法：以亚磷酸二乙酯和多聚甲醛经缩合、酯化得到对甲苯磺酸羟甲基磷酸二乙基酯（4）。另以缩水甘油合成碳酸丙烯酯，与腺嘌呤反应得到9-（2-羟丙基）腺嘌呤（7），在叔丁醇钠作用下与（4）经缩合、水解等反应制得抗病毒药物替诺福韦。结果：优化后的制备工艺成本低，操作简便，对环境污染减少。结论：新工艺的产率达到30％，适合工业生产。
|
| 关 键 词： | 替诺福韦 合成 工艺改进 |
| 收稿时间： | 2008/9/25 0:00:00 |
Improvement of synthetic process of tenofovir |
| |
| LIU Ji,LI Ke,SUN Hai-ling and FENG Ji-lu.Improvement of synthetic process of tenofovir[J].The Journal of Pharmaceutical Practice,2009,27(1):31-32,45. |
| |
| Authors: | LIU Ji LI Ke SUN Hai-ling and FENG Ji-lu |
| |
| Institution: | Department of Medicinal Chemistry, School of pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Medicinal Chemistry, School of pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Medicinal Chemistry, School of pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Medicinal Chemistry, School of pharmacy, Second Military Medical University, Shanghai 200433, China |
| |
| Abstract: | Objective: To improve the synthetic process of tenofovir.Methods: P-toluenesulfonic acid diethoxyphosphorylmethyl ester(4) was prepared from diethyl phosphate and paraformaldehyde by condensation and esterification.9-(2-hydroxy-propyl)adenine(7) was synthesized by reaction of adenine and propylene carbonate.In presence of(CH3)3CONa,compound(7) was connected with compound(4),and then hydrolyzed to tenofovir.Results:The technique was successfully improved due to its low cost,easier operation and less pollution to the environment.Conclusion: The overall yield of the improved synthetic process was 30%,which is more suitable for industrial production. |
| |
| Keywords: | tenofovir synthesis technical improvement |
| 本文献已被 维普 万方数据 等数据库收录！ |
| 点击此处可从《药学实践杂志》浏览原始摘要信息 |
| 点击此处可从《药学实践杂志》下载免费的PDF全文 |
|
