Study On The Improving Industrial Production Technique Of Zidovudine

Zidovudine(ZDV),also known as zidovudine(AZT),is an antiviral drug and a nucleoside reverse transcriptase inhibitor,which is a first anti-AIDS drug approved by the U.S.Food and Drug Administration.In recent years,the demand of Zidovudine increased because which was a medical for HIVpatients offered by governments.As a result,Zidovudine production is still in a state of insufficient supply and difficulty in meeting market demand.Recently,the price of zidovudine is declining due to the continuous improvement of the synthesis process and the reduced manufacturing costs,and this is the gospel of HIV patients.However,there is still some problems in the production of Zidovudine need to be overcome,such as low yield,high demanding conditions.Therefore,improving the conventional process,researching a new thchnque with higher yield,less pollution and less cost has attracted more attention.In this thesis,a new improved production process was proposed based on the original industrial production process using thymidine as raw material,which involved five-steps reaction:triphenyl protection,sulfonated,oxygen bridge,azide,and then hydrolysis.The main difference with the original synthetic route is using an oxygen bridge route to avoid twice sulfonation reaction,that thereby avoided the production of impurities-B,solved the control of azide reaction and improved the yield of zidovudine.While,the introduction of recycling triphenylmethyl protecting groups reduced the overall costs of zidovudine.Futhermore,a improved production route of zidovudine was designed and practiced,the main conditions were optimized and the industrial production program was proposed.The results of experiments and analysis showed that the price of the improved process was 1344 yuan/kg,which for original production process was 1745 yuan/kg.The cost advantage is more obvious for improve process.Because of reducing one-step reaction,the improved production process reduced the requirements for equipment and personnel,and the equipment costes also slow down.