Triaza-macrocyclic compounds, based on the pseudo-dilution effect on solid support, were designed and synthesized. The key building blocks for cyclization were two lysine residues and bromoacetic acid as the bridging components via acylation-S_N2 reaction in sequence. By present procedure, five target compounds 8, 9, 10, 12 and 13 with trinitrogen atoms in a 16-membered ring were obtained in good overall yields of 68.9%～86.1% and characterized by amino acid analysis and ESI-MS.

Key words: nitrogen containing macro-ring, peptide structure modification, solid-phase synthesis