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LIU Jia, LI Ke, SUN Hai-ling, FENG Ji-lu. Improvement of synthetic process of tenofovir[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(1): 31-32,45.
Citation: LIU Jia, LI Ke, SUN Hai-ling, FENG Ji-lu. Improvement of synthetic process of tenofovir[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(1): 31-32,45.

Improvement of synthetic process of tenofovir

  • Received Date: 2008-09-25
  • 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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    沈阳化工大学材料科学与工程学院 沈阳 110142

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Improvement of synthetic process of tenofovir

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.

LIU Jia, LI Ke, SUN Hai-ling, FENG Ji-lu. Improvement of synthetic process of tenofovir[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(1): 31-32,45.
Citation: LIU Jia, LI Ke, SUN Hai-ling, FENG Ji-lu. Improvement of synthetic process of tenofovir[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(1): 31-32,45.

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