西仑吉肽的合成制备

Synthesis and Preparation of Cilengitide

西仑吉肽(cilengitide)是一个含RGD序列人工改造设计得到的生物活性环肽,对整合素αvβ3具有较高的亲和性和选择性。本研究主要对西伦吉肽合成方法进行研究:采用固液相结合合成法,以二氯树脂为固相载体,以HBTU、PyBOP为缩合剂,固相合成线性肽后液相合成环肽,采用制备型反相高效液相色谱法进行纯化。产品纯度为98.3%,总收率为28.2%。该合成方法简单易行,产品纯度较高,适合用于西仑吉肽工业生产。

Cilengitide, a kind of bioactive cyclopeptide, is derived from the redesign of a sequence con- taining RGD and it has better affinity and selectivity for av/33. This article focused on the research of the synthesis of cilengitide ： combining the solid phase synthesis of the linear precursor and solvent phase syn- thesis of the cyclopeptide. Cilengitide was synthesized successfully with the raw material of Fmoc-amino acids and 2CTC- resin as vector, HBTU and PyBOP as coupling agents, and was purified with reverse phase high performance liquid chromatography. The purity of the refined peptide after purification was 98.3% and the overall yield was 28.2%. This method is very practical and applicable to the industrial manufacture.