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。
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 ）3 CONa, 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.
出处
《药学实践杂志》
CAS
2009年第1期31-32,45,共3页
Journal of Pharmaceutical Practice
关键词
替诺福韦
合成
工艺改进
tenofovir
synthesis
technical improvement
