作者:Spyridon Mourtas、Dimitrios Gatos、Kleomenis Barlos
DOI:10.3390/molecules24234261
日期:——
N-mercaptoalkylglycine residues were inserted into peptides by reacting N-free amino groups of peptides, which were initially synthesized on 2-chlorotrityl resin (Cltr) using the Fmoc/tBu method, with bromoacetic acid and subsequent nucleophilic replacement of the bromide by reacting with S-4-methoxytrityl- (Mmt)/S-trityl- (Trt) protected aminothiols. The synthesized thiols containing peptide–peptoid
N-巯基烷基甘氨酸残基通过使肽的 N-游离氨基与溴乙酸反应并随后通过与S-4-甲氧基三苯甲基-(Mmt)/S-三苯甲基-(Trt)保护的氨基硫醇。合成的含有肽-类肽杂化物的硫醇从树脂上裂解下来,要么通过用二氯甲烷 (DCM)/三氟乙醇 (TFE)/乙酸 (AcOH) (7:2:1) 处理保护,要么通过以下方式去保护(完全或部分)使用三乙基硅烷 (TES) 作为清除剂,用三氟乙酸 (TFA) 溶液处理。