Glushchenko A. Synthesis, physical-chemical properties and anticonvulsant activity of the 1-aryl-4-R-5methyl(amino)-1,2,3-triazole(1H)derivatives

The target-directed synthesis of the potential anticonvulsants among the 1-aryl-4-R-5-methyl(amino)-1,2,3-triazole(1H) was carried out. The preparative methods of synthesis of the new groups of biologically active compounds were designed: for the anilides of the 1-R-5-methyl-1,2,3-triazole(1H)-4-carboxylic acid – by interaction of the acetoacetic acid amides with the aryl azides under the homoge-nous basic catalysis conditions; the 1-R-5-methyl-4-arylsulfonyl-1,2,3-triazoles(1H) – by the reaction of the aryl azides and the aryl sulfonyl acetones in the system methanol/sodium methanolate; the 1-R-4-arylsulfonyl-5-amino-1,2,3-triazoles (1H) – by the reaction of the aryl sulfonyl acetonitriles with aromatic azides. The thermal isomerization of 5-amino derivatives into 5-aryl amino derivatives was carried out. The structures of the synthesized compounds were confirmed by the elemental analysis, IR-, UV- and HNMR-spectroscopy’s data. The pharmacological screening showed the number of perspective anticonvulsants. For the most active one – 3-chloro-4-methoxy anilide of the 1-(2’-fluorophenyl)-5-methyl-1,2,3-triazole(1H)-4-carboxylic acid the project of AND was developed.