Abstract Cilengitide, a kind of bioactive cyclopeptide, is derived from the redesign of a sequence containing RGD and it has better affinity and selectivity for αvβ3. This article focused on the research of the synthesis of cilengitide: combining the solid phase synthesis of the linear precursor and solvent phase synthesis of the cyclopeptide. Cilengitide was synthesized successfully with the raw material of Fmocamino 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.
KONG Yi, HUANG Hai, LAI Yi-Li, HUANG Shi-Long, LIU Hui-Min.Synthesis and Preparation of Cilengitide[J] Chemcial Industry and Engineering, 2012,V29(4): 33-37
2012, Vol. 29 
