多肽C端衍生物的反向固相合成新方法

Novel synthesis of C-terminal polypeptides by ISPPS method

新设计了一种多肽C-端衍生物的合成方法。本方法结合了Fmoc-SPPS技术与TAEC技术的优点,室温反应,反应条件温和,易于监测,反应过程中所需采取的保护基最少,后处理简单高效,与正向固相合成互补,可高效地合成多种多肽以及多肽C-端衍生物。

A facile approach for the preparation of polypeptide C-terminal derivatives by inverse solid phase peptide syn- thesis （ISPPS） was developed. This novel method combines both advantages of Fmoc-SPPS and TAEC technology, utilizes fewer functional group protection steps. In addition, the reaction can be carried out at room temperature under mild conditions and be easily monitored, and the working-up is simple and efficient. This method is complementary to the direct solid phase peptide synthesis. Several polypeptides as well as their C-terminal derivatives were efficiently pre- pared by this novel ISPPS method.