| 甲烷磺酸N-羟基琥珀酰亚胺酯的制备及其在寡肽合成中的应用 |
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| 引用本文： | 张江峰,孟庆国,毛扬,孙海军,梁月洁.甲烷磺酸N-羟基琥珀酰亚胺酯的制备及其在寡肽合成中的应用[J].烟台大学学报(自然科学与工程版),2009,22(1). |
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| 作者姓名： | 张江峰 孟庆国 毛扬 孙海军 梁月洁 |
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| 作者单位： | 烟台大学,药学院,山东,烟台,264005 |
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| 基金项目： | 烟台大学校科研和教改项目 |
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| 摘 要： | 制备甲烷磺酸N-羟基琥珀酰亚胺酯,并将其应用于寡肽的液相合成.以N-羟基琥珀酰亚胺与甲烷磺酰氯反应制备甲烷磺酸N-羟基琥珀酰亚胺酯,并使其与Boc保护的酪氨酸、丙氨酸或Boc保护的酪氨酰脯氨酸发生SN2取代反应,生成相应的N-羟基琥珀酰亚胺活泼酯而活化羧基,并成功用于内吗啡肽-2和力肽的液相合成;N-羟基琥珀酰亚胺活泼酯的制备和应用反应条件温和、副产物少、收率较高.实验结果表明,甲烷磺酸N-羟基琥珀酰亚胺酯可用于寡肽的液相合成.
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| 关 键 词： | 甲烷磺酸N-羟基琥珀酰亚胺酯 合成 活泼酯 寡肽 |
Preparation of Methanesulfonyl N-hydroxysuccinate and Its Application in Synthesis of Oligopeptides |
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| ZHANG Jiang-feng,MENG Qing-guo,MAO Yang,SUN Hai-jun,LIANG Yue-jie.Preparation of Methanesulfonyl N-hydroxysuccinate and Its Application in Synthesis of Oligopeptides[J].Journal of Yantai University(Natural Science and Engineering edirion),2009,22(1). |
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| Authors: | ZHANG Jiang-feng MENG Qing-guo MAO Yang SUN Hai-jun LIANG Yue-jie |
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| Institution: | ZHANG Jiang-feng; MENG Qing-guo; MAO Yang; SUN Hai-jun; LIANG Yue-jie(School of Pharmacy; Yantai University; Yantai 264005; China); |
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| Abstract: | The preparation of methanesulfonyl N-hydroxysuccinate and its use in the synthesis of oligopeptides in liquid phase has been studied.Methanesulfonyl N-hydroxysuccinate is synthesized from methanesulfonyl chloride and N-hydroxysuccimide,and used to prepare activated esters of N-Boc-Tyr-OH,N-Boc-Ala-OH,N-Boc-Tyr-Pro-OH by SN2 substituted reaction.In this study,methanesulfonyl N-hydroxysuccinate is successfully used in the synthesis of endomorphine-2(EM-2) and alanylglutamine.All the reactions can be operated under mild conditions with less side reaction and in high yield.The results show that methanesulfonyl N-hydroxysuccinate can perfectly meet the performance of oligopeptide synthesis in liquid phase. |
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| Keywords: | methanesulfonyl N-hydroxysuccinate synthesis activited ester oligopeptide |
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