软刀素肽的固相合成

Solid-phase synthesis of urumin

目的制备抗H1型病毒的软刀素肽。方法采用9-芴甲氧羰基（Fmoc）固相合成法，选用Wang树脂为载体，以HOBt／DIC为缩合试剂依次偶联氨基酸后，将多肽从树脂上切割下来，得到的粗品采用制备HPLC进行纯化。结果制得纯度〉98．2％的多肽产物，用HPLC归一化法测定的含量为26．3％，所得产物通过HRMS分析，确定为软刀素肽。结论所用方法可行性高、操作简便，收率较高，目标化合物可用于抗H1型病毒的后续药物研究。

OBJECTIVE To synthesize urumin, the peptide used to treat human H1 hemagglutinin -bearing influenza virus. METHODS Aided by solid -phase peptide synthesis（SPPS） , the peptide was synthesized with Wangresin as the solid supporter. The amino acids were immobilized accordingly with HOBt/DIC as coupling regents, and then the crude product was cut from the resin and purified by preparative RP - HPLC. RESULTS The title compound was obtained and characterized by HPLC （ purity 〉 98.2% ） and HRMS, with HPLC normalized yield of 26.3 %. CONCLUSION This synthetic method is demonstrated as a feasible and effective synthetic method, and the resulted peptide can be applied to the research of the anti - H1 influenza viruses drug.