To optimize the synthetic process of tenofovir,we synthesized tenofovir using adenine and(R)-propylene carbonate as starting materials through ring-opening condensation,substitution and hydrolysis.The processes of reactions were monitored by using high performance liquid chromatography.The best synthesis conditions for ring-opening condensation and substitution reaction were at 120℃for 22 h and at 60℃for 6 h,respectively.The best reaction time of hydrolysis is 20 h.The total yield is 69.2％under optimal conditions.The photophysical properties were investigated by UV-vis absorption spectroscopy and fluorescence emission spectroscopy,and the direction and extent of reaction can be monitored according to the wavelengths of fluorescence emission of different compounds.Tenofovir shows certain antibacterial activities against Staphylococcus aureus at a low concentration.This synthetic process realizes the by-product recovery and application,saves the production cost,and improves the production capacity.
关键词
替诺福韦/高效液相色谱法中控/荧光监测/工艺优化/抗菌活性
Key words
tenofovir/HPLC central control/fluorescence monitoring/process optimization/antibacterial activity
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