ИСТИНА

Many currently notable drugs contain a piperazine ring as part of their molecular structure: analgesics, muscle relaxants, аntidepressants, аntihistamines, аntipsychotics (frenolon, triftazine) and some of the antitumoral drugs (dipine, prospidine, spirazipine). At the same time about 25% of all drugs produced to date contains in their structure at least one atom of fluorine or trifluoromethyl group. However, the direct fluorination of complex compounds with multiple functional groups is often impossible for many reasons. Effective way of synthesis of fluorinated piperazines with various substituents on nitrogen and carbon atoms is relevant for the development. We suggest that the aza-Henry reaction between CF3-substituted ketimines and number of nitroalkanes with further reduction to 1,2- diamines and addition of 1,2-dibromethane could lead to the fluorinated piperazines at multipurpose and simple way. Using variation of ketimines, containing removable protecting groups, and nitroalkanes can provide a plenty amount of different piperazine-cored structure types.