本文报道了在合成天然的蛋白酶体抑制剂Syringolin A(SylA)及其类似物的过程中,首先合成的两种类型的SylA开环类似物。经过7步反应,第一种类型产物总收率在20%-34%之间,第二种类型产物总收率在12%-18%之间。与SylA相似,这两种类型的类似物也都具有肽乙烯酰胺的结构,可能作为Michael受体与蛋白酶体催化活性位点ThrlO~γ发生1,4-加成反应,从而发挥蛋白酶体抑制活性。 We report the first two types of SylA open-loop analogues synthesized in the synthesis of the natural proteasome inhibitor Syringolin A (SylA) and its analogues. After 7 steps, the total yield of the first type of product is between 20% and 34%, and the total yield of the second type product is between 12% and 18%. Similar to SylA, both types of analogues also have the peptide-vinyl amide structure that may act as a proteasome inhibitory activity by acting as a 1,4-addition reaction between the Michael acceptor and the catalytic site of the proteasome ThrlO ~ γ .