| 替诺福韦的合成工艺改进 |
| 投稿时间：2008-09-25 点此下载全文 |
| 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 |
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| 中文摘要: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。 |
| 中文关键词:替诺福韦 合成 工艺改进 |
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| Improvement of synthetic process of tenofovir |
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| 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 |
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