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自组装多功能反应器固相合成依非巴特
引用本文:绳则翠,周成,张龄之,朱亮亮,姜波,陈英文,祝社民,沈树宝.自组装多功能反应器固相合成依非巴特[J].应用化学,2012,29(3):275-279.
作者姓名:绳则翠  周成  张龄之  朱亮亮  姜波  陈英文  祝社民  沈树宝
作者单位:(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)
基金项目: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
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  
收稿时间:2011-05-26

Solid-phase Synthesis of Eptifibatide in a Multifunctional Reactor
SHENG Zecui , ZHOU Cheng , ZHANG Lingzhi , ZHU Liangliang , JIANG Bo , CHEN Yingwen , ZHU Shemin , SHEN Shubaoa.Solid-phase Synthesis of Eptifibatide in a Multifunctional Reactor[J].Chinese Journal of Applied Chemistry,2012,29(3):275-279.
Authors:SHENG Zecui  ZHOU Cheng  ZHANG Lingzhi  ZHU Liangliang  JIANG Bo  CHEN Yingwen  ZHU Shemin  SHEN Shubaoa
Institution:(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)
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%.
Keywords:Eptifibatide  solid-phase synthesis reactor  Fmoc method
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