Synthesis Of 7-amino-5-hydroxy-2-methyl-pyrazolo[1,5-a]pyrimidine Derivatives And 5-amino-pyrazolo[1,5-a]pyrimidine-2,7-diol

Objective In tumor cells the metabolic speed is faster than in normal cells, the synthesis of nucleic acids also in large quantities. In vivo, the metabolism of drugs inhibit the later stage synthesis of DNA, and they have the ability to interference or interrupt the biosynthesis of DNA and protein. In our subject, we designed and synthesized a suite of purine analogue, expecting to screening the lead compounds which have the antitumor effectiveness. Methods In sodium ethoxide solution, 7-amino-5-hydroxy-2-methyl-pyrazolo[1,5-a]pyrimidine(compound 2) was synthesized from the reaction of 3-amineyl-5-methyl-2H-pyrazol and ethyl cyanoacetate, and compound 2 reacted with a suite of aromatic diazonium chlorides, 7-imino-5-hydroxy-2-methyl-6-phenylazo-pyrazolo[1,5-a]pyrimidine derivatives were synthesized. Ethyl cyanoacetate reacted with hydrazine synthesized cyanoacetohydrazide,cyanoacetohydrazide cycling in sodium methylate solution synthesized 3-amino-5-hydroxypyrazole(compound 4), compound 4 reacted with ethyl cyanoacetate synthesized5-amino-pyrazolo[1,5-a]pyrimidine-2,7-diol. All the compounds were identified by 1H-NMR/13 C NMR thin-layer, mass spectrometry(MS), infrared(IR) and chromatography(TLC).Results Eleven purine analogues were synthesized, ten compounds are new purine analogue.Conclusion The structure of the target compounds were confirmed by the spectroscopic methods mentioned above. The pharmacological activity of target compounds are under way.