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The most wide spread drugs are those, which contain in their structures heterocyclic fragment. Such trend could be explained by the fact that, heterocycle containing compounds are the part of the number of substances, which play an important role in the metabolic processes. It should be noted, that most of these drugs have unpleasant side effects and some of them are rather toxic. Xanthine derivatives are low toxic natural compounds with wide spectrum of pronounced pharmacological properties (antioxidant, diuretic, antibacterial, anti-infl ammatory etc.) and high variability of chemical modifi cation, that make these compounds handy objects for pharmaceutical research. Thus, synthesis of novel less toxic biologically active compounds – potential medicines – by chemical modifi cation of well-known natural substances, is one of the most important tasks of modern pharmaceutical science. It is of great significance to develop synthetic methods for 3-aryl(aralkyl)-8-hydrazinemethylxanthines and their N-substituted derivatives and study their physical and chemical properties.