ИСТИНА

The introduction of α-CF3-α-amino acid derivatives into peptides by conventional methods of peptide chemistry is not a trivial task. Due to the low nucleophilicity of the amino-function and steric effects of the СF3- group in α-trifluoromethyl α-amino acids the modification of standard methods for the peptide synthesis is required. On the other hand, triazole-containing derivatives are attractive drug candidates because they could be easily prepared via selective copper (I)-catalysed cycloaddition reaction known as “click” reaction between decorated functionally azides and alkynes. Moreover triazole ring is a known bioisoster of peptide bond possessing high stability towards proteolysis. Thus, we present a convenient synthetic pathway to novel functionalized tetrapeptides comprising triazole moiety as a linker connecting fluorinated α-amino acids and α-aminophosphonates with functionally substituted azidopeptides. As well as we suggest an efficient and simple synthetic approach to novel α-CF3-containing triazolyl α-amino acids and α-aminophosphonates as potential neurotransmitters.