O,N-Glycosylation reactions are used for the synthesis of prodrugs based on various pharmaceutical substances. This, in turn, can significantly improve their pharmacokinetic and pharmacodynamic parameters, as well as reduce toxic effects. In current study, the objective was to propose new variants of the synthesis of active glycosylating agents, superior to the previously known ones in terms of the use of highly toxic substances, the anomeric composition of the products and the reaction time.