A chiral five-membered ring α, α-disubstituted α-amino acid (R, R)-Ac5cdN3 having two azido functional groups has been designed and synthesized. The cyclic amino acid (R, R)- Ac5cdN3 could be efficiently converted into several cyclic amino acids with various two 1, 2, 3-triazole functional groups.(R, R)-Ac5cdN3 homochiral peptides (up to hexapeptide) and (R, R)-Ac5cdN3-containing l-Leu-based peptides were prepared, and their conversion of ...