基于蛋白酶体抑制剂作为麦克尔加成反应的受体参与对蛋白酶体抑制作用的机制,我们设计并合成了6个二肽乙烯磺胺类化合物,并对它们的酶抑制活性与细胞抑制活性进行研究。同时,在合成这类化合物的过程当中,我们找到了一种有效的利用维悌希反应作为关键步骤来合成g-氨基乙烯磺胺中间体的方法,为肽乙烯磺胺类化合物的方便及多样性合成提供了有效途径。 Based on the mechanism that proteasome inhibitor acts as a receptor for Michael Addition reaction in proteasome inhibition, we designed and synthesized six dipeptide ethanesulfonamides and studied their enzyme inhibitory activity and cytostatic activity . At the same time, during the synthesis of these compounds, we have found an efficient method for the synthesis of g-aminoethanesulfonamide intermediates using the Wittig reaction as a key step for the convenient and diverse synthesis of peptide-vinyl sulfonamides Provide an effective way.