.2,6,8 - Three Mercaptopurine Synthesis Study

Purine derivatives are a kind of antiviral drugs and a kind of pharmaceutical intermediate in preparation nucleotide. Some substitution groups are introduced to 2,6,8-substitue of purines, Thus, these purines have the biomedicine activity of antiviral, anticancer and dropping blood pressure.2,6,8-purinetrithiol was obtained by using methyl cyanacetate as starting material via five steps reaction of cyclization, nitrosylation, reduction, closed ring action and thionation. 4-amino-6-hydroxy-2-mercapto-pyrimidine was prepared from methy1 cyanacetate by the reactions of cyclization, adding sodium methylate and thiourea to it. Then synthesized 4-amino-5-nitroso-6-hydroxy-2-mercaptopyrimidine by the reaction of nitrosylation. Using sodium dithionite deoxidized 4-amino-5-nitroso-6-hydroxy-2-mercaptopyrimidine,then obtained 4,5-diamino-6-hydroxy-2-mercaptopyrimidine. 6-hydroxy-2,8-purinedithiol was prepared by the reaction of closed ring action, adding carbon disulfide to it. Finally, 2,6,8-purinetrithiol was obtained by the reaction of thionation , adding phosphorus pentasulfide. And the overall yield is 54.3%. This dissertation made a research on the following factors such as reaction temperature, time and dosage of all kinds of materials. After the dissertation introduce single factor to consurmnate the technological process and technological condition. The structures and compounds were determined by IR, HPLC and LC-MS spectra.