Peptide modification by introduction ofα-trifluoromethyl substituted amino acids.

Methodology for the synthesis and incorporation ofα-trifluoromethyl substituted amino acids into N- and C-terminal position of peptides is described. The incorporation ofα-trifluoromethyl substituted amino acids into strategical positions of peptides enhances proteolytic stability and lipophilicity. Furthermore, it improves transport rates in vivo and permeability through certain body barriers.