Research On The Craft Of Tenofovir

Tenofovir, the chemical name of which is R-9-(2-phosphoric methoxypropyl) adenine, isthe key intermediate of the antivirals of tenofovir disoproxil fumarate. Fumarate listingalternate tenofovir ester2001was approved by the FDA for the treatment of HIV-infectedpatients, a new open-loop nucleotide class of anti-HIV drugs, which also has the role ofanti-hepatitis virus infection, has broad market prospects.This article is aimed at improving research on alternative the tenofovir synthetic routesand synthesis process for the synthesis of the adenine tenofovir production technology, toimprove product yield. Comprehensive reaction conditions are such as temperature, reactiontime, and determine its industrialization conditions.Firstly, the research on synthesizing magnesium tert-butoxide, their production can bevery effective reducing production costs. This paper used the ester exchange method, usingtetrabutyl titanate as the catalyst by addition of acetic acid tert-butyl ester and toluene mixedsolvent, distillating8h final achieved purity of95%magnesium tert-butoxide, and got goodresults in the subsequent reaction of use. Tosyloxy methylphosphonate synthesis, identifiedby the triethylamine as a catalyst and the second-stage reaction in the first reaction step of theacid-binding agent, and improved purification process to improve the yield of the two stepyield of68.5%.(1) R-9-(2-hydroxypropyl) adenine synthesis process inspection, determine the reactiontemperature100℃, the molar ratio of1:1.2,as the molar ratio of adenine and R-propylenecarbonate is1:1.2, and the reaction time is6h,get the highest yield of the product. Under thiscondition, we minimize the production of by products, and improve the yield to83.0%.(2)R-9-[2-(diethoxy phosphono-methoxy) propyl] adenine synthesis process to determine theoptimum reaction conditions, and the reaction time is3h, and the reaction temperature is60℃,and the holding time is1.5h.The yield of the product is90.1%. Examine alternative oftenofovir synthesis process, determine the dropping temperature of10℃, the holding time of8h, holding temperature of55℃, the yield is up to91.2%. The structure of the product wasanalysed by1H-NMR, IR.