Trivalent organoarsenic compounds have attracted a great deal of interest because of their potential antineoplastic activities. In this work, we synthesized a series of arsenic-containing amino acid analogues by introducing the structure of 1-arsino-2,6,7- trithiobicyclo[2.2.2]octane to the side chain of modified amino acid derivatives. The protected amino acid （6a） as a typical objective compound was applied in peptide synthesis via the classic procedures for the formation of peptide bond or removal of protecting groups. Our results showed that the application of compound 6a （or 5a） in the peptide chemistry was satisfactory.
