中文摘要：

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Ⅳ一溴代琥珀酰亚胺／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。

英文摘要：

N＇-Phenylacylhydrazide safly-catch resin was syn- thesized by derlvatizing commercial available MBHA resin with N＇-Boc-4-hydrazinobenzoic acid. N＇-Protection form of 4- hydrazinobenzoic acid and initial amino functional resin type have been investigated to achieve higher derivation yield. Five serine protease peptidyl-pNA chromogenic substrates were synthesized with the safty-catch resin by Boc/Fmoc hybrid- ized protocol with high yields and purity. Intermediates and product were characterized by HRMS and NMR.