肽基环氧酮类化合物对20S蛋白酶体具有抑制作用, 使之成为可能的抗肿瘤药物。根据此类抑制剂的结构和特殊抑制机理,我们设计了一系列连接环氧酮部分(C-末端药效团) 和肽骨架的化合物。合成工作方面, 我们使用了经过Weinreb酰胺得到关键中间体末端α,β-不饱和酮的新合成方法, 产率为62%-65%。 Peptide-based epoxy ketones have an inhibitory effect on the 20S proteasome, making it an antitumor drug. Based on the structure of this class of inhibitors and the specific inhibitory mechanism, we have designed a series of compounds that link the epoxy ketone moiety (the C-terminal pharmacophore) and the peptide backbone. For the synthesis work, we used a novel synthesis of α, β-unsaturated ketones via Weinreb amide at the key intermediate end with a yield of 62% -65%.