Synthesis of 2,5,7-triamino[1,2,4]triazolo[1,5- a ][1,3,5]triazines as potential antifolate agents

The synthesis of 2,5,7-triamino[1,2,4]triazolo[1,5-a][1,3,5]triazines was developed. The 3,5-diamino-1,2,4-triazoles were prepared using partial aminolysis of dimethyl N-cyanodithiocarbonimidate followed by cyclization of the obtained N-substituted N’-cyano-S-methylisothioureas with hydrazine. The reaction of 3,5-diamino-1,2,4-triazoles with cyanoguanidine was found to afford 2,5,7-triamino[1,2,4]triazolo[1,5-a][1,3,5]triazines. The structure of the compounds obtained was established using NMR spectroscopy.