Preparation Of2,5-diamino-4,6-dihydroxypyrimidine Hydrochloirde

AIDS is the infectious disease caused by the infection of human immunodeficiencyvirus. Since the first report of AIDS in the United States in1981, AIDS has quicklyspread and diffused within the scope of the whole world. Due to the lack of a cure forAIDS, the infectors are gradually led to death with fear. So AIDS is named "super cancer"and "century plague". Aids is in no way a simple medical problem, but a serious andheavy-loaded social problem because of the expensive treatment.At present the better treatment of AIDS is the therapy of “cocktail”, which has acertain control of the morbidity and mortality of AIDS. Abacavir is the essential medicinein the therapy of “cocktail”, which has the features of high oral bioavailability, access tocentral nervous system, slow drug resistance. Therefore, the research of Abacavir hassubstantial significance to the treatment of AIDS.This thesis mainly focuses on the Preparation of2,5-diamino-4,6-dihydroxypyrimidine, the important intermediate products in the building-up process of Abacavir. Atfirst, based on the best synthetic route worked out through lots of literatures and thedescription in the literatures, an experiment was conducted and the yields of the finalproducts were not ideal. Then the experiment condition of the reaction was improved afterthe research and analysis of the synthetic route for the reaction mechanism. The optimalreaction condition for the preparation of2-amino-4,6-dihydroxyprimidine and2-amino-4,6-dihydroxy-5-nitroso primidine was confirmed through comparisonexperiment. The yields of the two intermediate products were improved by25%and20%.The project design was conducted through orthogonal experimental design method for theinfluencing factors of the reacting of2,5-diamino-4,6-dihydroxypyrimidine. The data wasprocessed with range analytical procedure. The primary and secondary order of theinfluencing factors to the conversion of final products was found:The varieties of organic solvent> the concentration of sodium hydroxide> thereaction temperature> the dosage of catalyst. The optimal synthetic conditions are:“takeethanol as the organic solvent, control the temperature at20℃, the dosage of catalyst0.4g,the concentration of sodium hydroxide0.2mol/L, and the reaction time30hours.” Underthese conditions the conversion rate of the final product can reach88.7%.