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自组装多功能反应器固相合成依非巴特

绳则翠1,周成1,张龄之3,朱亮亮1,姜波1,陈英文1,祝社民2,沈树宝1*   

  1. (1.南京工业大学生物与制药工程学院 南京 210009；2.南京工业大学材料科学与工程学院 南京;
    2.徐州师范大学化学化工学院 徐州)
  • 收稿日期:2011-05-26 修回日期:2011-07-12 出版日期:2012-03-10 发布日期:2012-03-10
  • 通讯作者: 沈树宝，教授; Tel:025-58139922; Fax:025-58139369; E-mail:zsbshen@njut.edu.cn; 研究方向：多肽合成、酶工程及环境工程
  • 基金资助:
    国家863资助项目(2009AA05Z313，2006AA02Z211)，国家自然科学基金资助项目(50872052,20376034)，江苏省自然科学基金资助项目(BK2006181)，江苏省高校研究生创新计划资助项目(2007)，江苏省环保厅资助项目(2009002)，江苏省科技厅资助项目(BE2010196)，江苏高校优势学科建设工程资助项目

Solid-phase synthesis of Eptifibatide in a multifunctional reactor

SHENG Zecui1, ZHOU Cheng1, ZHANG Lingzhi3, ZHU Liangliang1, JIANG Bo1, 
CHEN Yingwen1, ZHU Shemin2, SHEN Shubao1*   

  1. (1.College of Biotechnology and Pharmaceutical Engineering,Nanjing University of Technology,Nanjing 210009;
    2.College of Material Science and Engineering,Nanjing University of Technology,Nanjing;
    3.Chemistry and Chemical Engineering Department,Xuzhou Normal University,Xuzhou)
  • Received:2011-05-26 Revised:2011-07-12 Published:2012-03-10 Online:2012-03-10

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摘要： 采用集反应、搅拌、鼓泡、N2气保护和过滤五重功能的自组装反应器，研究了树脂种类、溶剂、缩合试剂和反应时间对环肽依非巴特产率的影响。 结果表明，以Rink Amide AM树脂为固相载体，HBTU/HOBt/DIEA为肽键缩合剂，DMF为溶剂，反应2 h，粗肽得率高达86.6%，经液相色谱纯化后纯度达98%以上。

关键词: 依非巴特, 固相合成反应器, Fmoc法

Abstract: A home-made reactor possessing functions including reaction, blending, bubbling, protecting with N2 and filtration was fabricated. The effects of the type of resin, solvent, coupling reagent and reaction time on the yield of cyclic eptifibatide were investigated. The results showed the overall yield was up to 86.6%, using Rink Amide AM resin as solid supporter, HBTU/HOBt/DIEA as the coupling reagent, DMF as the solvent and reaction 2 hours in the reactor. The purity of the product as revealed by HPLC could reach 98%.

Key words: Eptifibatide, Solid-phase synthesis reactor, Fmoc method

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