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化学工业与工程 2012, Vol. 29 Issue (4) :33-37    DOI:
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西仑吉肽的合成制备
 孔毅, 黄海, 赖伊丽, 黄世龙, 刘会敏
(中国药科大学生命科学与技术学院,江苏 南京 210009)
Synthesis and Preparation of Cilengitide
 KONG  Yi, HUANG  Hai, LAI  Yi-Li, HUANG  Shi-Long, LIU  Hui-Min
(School of Life Science & Technology, China Pharmaceutical University, Nanjing 210009, China)

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摘要 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。
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孔毅
黄海
赖伊丽
黄世龙
刘会敏
关键词西仑吉肽   固相合成   液相合成     
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 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.
Keywordscilengitide   solid phase synthesis   solvent phase synthesis     
引用本文:   
孔毅, 黄海, 赖伊丽, 黄世龙, 刘会敏.西仑吉肽的合成制备[J].  化学工业与工程, 2012,29(4): 33-37
KONG Yi, HUANG Hai, LAI Yi-Li, HUANG Shi-Long, LIU Hui-Min.Synthesis and Preparation of Cilengitide[J].  Chemcial Industry and Engineering, 2012,29(4): 33-37
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