| 赖氨酸衍生氮杂大环化合物的固相合成 |
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| 引用本文： | 杨潇骁,邱传亮,王德心.赖氨酸衍生氮杂大环化合物的固相合成[J].有机化学,2005,25(6):712-715. |
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| 作者姓名： | 杨潇骁 邱传亮 王德心 |
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| 作者单位： | 中国医学科学院药物研究所,北京,100050 |
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| 基金项目： | 高等学校博士学科点专项科研项目 |
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| 摘 要： | 基于固相载体的假稀释效应, 设计并合成了由赖氨酸为前体结构衍生的氮杂大环化合物8, 9, 10, 12及13. 合成中的关键构件是在固相树脂上肽链的N端键合的二个相邻的赖氨酸残基, 并以溴乙酸为桥连组份, 先后经酰化及亲核取代(SN2)反应完成三氮杂十六元环骨架的构建. 5种粗产物的总收率在68.9%～86.1%之间, 并全部经氨基酸组成分析及ESI-MS分析表征.
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| 关 键 词： | 氮杂大环 固相合成 肽结构改造 |
| 收稿时间： | 2004-6-25 |
| 修稿时间： | 2004年6月25日 |
Solid-phase Synthesis of Aza-macrocyclic Compounds Derived from Lysine Residues |
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| YANG,Xiao-Xiao,QIU,Chuan-Liang,WANG De-xin.Solid-phase Synthesis of Aza-macrocyclic Compounds Derived from Lysine Residues[J].Chinese Journal of Organic Chemistry,2005,25(6):712-715. |
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| Authors: | YANG Xiao-Xiao QIU Chuan-Liang WANG De-xin |
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| Institution: | (Institute of Materia Medica, Chinese Academy of Medical Science, Beijing 100050) |
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| Abstract: | Triaza-macrocyclic compounds, based on the pseudo-dilution effect on solid support, were designed and synthesized. The key building blocks for cyclization were two lysine residues and bromoacetic acid as the bridging components via acylation-SN2 reaction in sequence. By present procedure, five target compounds 8, 9, 10, 12 and 13 with trinitrogen atoms in a 16-membered ring were obtained in good overall yields of 68.9%～86.1% and characterized by amino acid analysis and ESI-MS. |
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| Keywords: | nitrogen containing macro-ring solid-phase synthesis peptide structure modification |
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