含砷氨基酸的合成及其在多肽化学中的应用

摘要

三价有机砷化合物以其潜在的抗肿瘤活性正在引起药物化学家的兴趣.本文中合成了一组在侧链上引入1-砷-2,6,7-三硫二环(2,2,2)辛烷结构单元的含砷氨基酸衍生物.以所合成的新型氨基酸的代表性化合物6a为例,将其用于多肽合成的应用中.此新型氨基酸在多肽的偶联、保护基的脱除等化学实验中表现良好的应用结果.%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.