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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 (cilengitide) is a bioactive cyclic peptide designed by artificial modification with RGD sequence and has high affinity and selectivity for integrin αvβ3. In this study, we mainly studied the synthesis of sero-ghrelin: the solid-liquid phase synthesis method, the dichlorinated resin as the solid phase carrier, the HBTU and PyBOP as the condensing agent, Purification by preparative reverse-phase high performance liquid chromatography. The purity of the product was 98.3% with a total yield of 28.2%. The synthesis method is simple and easy, the purity of the product is high, and is suitable for the industrial production of Cilengitide.