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针对液相合成对羧基苯胺发色底物的不足,采用Boc-对羧基苯肼和MBHA树脂为原料合成了具有保险拉手型连接臂结构的树脂,对保护基形式及树脂载体类型的选择进行了探讨。基于该型树脂采用微波辅助的Fmoc/Boc混合策略在树脂上合成了5个用于丝氨酸蛋白酶活性实验的多肽中间体,经温和的N-溴代琥珀酰亚胺/吡啶条件氧化连接臂后,与对硝基苯胺(pNA)发生氨解反应,以较高的收率和纯度得到5个丝氨酸蛋白酶发色底物。中间体及产物经过高分辨质谱和核磁共振氢谱确定了结构。
Aiming at the deficiency of liquid phase synthesis of carboxyaniline chromogenic substrate, Boc-p-carboxyphenylhydrazine and MBHA resin were used as raw materials to synthesize the structure of the handle with the structure of the insurance handle. The choice of protecting group and resin carrier type Discussion. Based on this resin, five peptide intermediates for serine protease activity were synthesized on the resin by microwave-assisted Fmoc / Boc mixed strategy. After the linker was oxidized by mild N-bromosuccinimide / pyridine, Anammolytic reaction with p-nitroanilide (pNA) resulted in 5 serine protease chromogenic substrates with higher yield and purity. Intermediates and products were identified by high-resolution mass and nuclear magnetic resonance spectroscopy.