| 第 36 卷第 1 期 |  | Vol. 36 No. 1 | | 2006 年 2 月 | Feb 2006 |
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所属栏目：医药及中间体
氨基化单甲氧基聚乙二醇的合成研究 |
| 王孝杰; 孙建平; 李效东; 刘克良(国防科技大学航天与材料工程学院; 军事医学科学院毒物药物研究所; 湖南长沙) |
| 摘 要：首先合成了单甲氧基聚乙二醇对甲苯磺酸酯(mPEG-OTs),然后根据盖布瑞尔合成法原理,以邻苯二甲酰亚胺钾盐(PPI)为亲核试剂与mPEG-OTs反应,生成单甲氧基聚乙二醇的邻苯二甲酰亚胺衍生物(mPEG-PI),mPEG-PI与水合肼反应肼解生成伯胺,合成了一端为氨基的单甲氧基聚乙二醇(mPEG-NH2)。讨论了缚酸剂、溶剂、反应条件对反应的影响。通过红外、液质联用、核磁共振谱图证实了产物与目标分子的结构相吻合。 |
| 关键词：聚乙二醇; 氨基化; 盖布瑞尔合成法; 合成 |
| 中图分类号：TQ325 文献标识码：A 文章编号：1009-9212(2006)01-0040-03 |
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| Synthesis of Amino-monomethoxypoly(ethy1ene glycol) |
| WANG Xiao-jie;SUN Jian-ping;LI Xiao-dong;LIU Ke-liang(College of Aerospace and Material Engineering;National University of Defense Technology;Changsha 410073;China;Institute of Pharmacology & Toxicology;Academy of Military Medical Science) |
| Abstract：Amino-monomethoxypoly(ethy1ene glycol)(mPEG-NH2) was synthesized based on the principle of Gabriel synthesis.Monomethoxypoly(ethy1ene glycol) tosylate(mPEG-OTs) was prepared at first,and then reaction with potassium salt of phthalimide(PPI) as nucleophile to produce the monomethoxypoly(ethy1ene glycol)phthalimide derivative(mPEG-PI).At last,the mPEG-PI and carboxamide hydrazine reacted to give the primary amine,and hydrolyzed to the target product mPEG-NH2.And the influences of reaction conditions such as s... |
| Key words：poly（ethylene glycol）; amino-; Gabriel synthesis; synthesis |
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收稿日期：2005-09-08
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