替诺福韦的合成工艺改进
Improvement of synthetic process of tenofovir
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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。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.
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Key words:
- tenofovir /
- synthesis /
- technical improvement
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