| 第 36 卷第 1 期 |  | Vol. 36 No. 1 | | 2006 年 2 月 | Feb 2006 |
|
所屬欄目：醫藥及中間體
氨基化單甲氧基聚乙二醇的合成研究 |
| 王孝杰; 孫建平; 李效東; 劉克良(國防科技大學(xué)航天與材料工程學(xué)院; 軍事醫學(xué)科學(xué)院毒物藥物研究所; 湖南長(cháng)沙) |
| 摘 要：首先合成了單甲氧基聚乙二醇對甲苯磺酸酯(mPEG-OTs),然后根據蓋布瑞爾合成法原理,以鄰苯二甲酰亞胺鉀鹽(PPI)為親核試劑與mPEG-OTs反應,生成單甲氧基聚乙二醇的鄰苯二甲酰亞胺衍生物(mPEG-PI),mPEG-PI與水合肼反應肼解生成伯胺,合成了一端為氨基的單甲氧基聚乙二醇(mPEG-NH2)。討論了縛酸劑、溶劑、反應條件對反應的影響。通過(guò)紅外、液質(zhì)聯(lián)用、核磁共振譜圖證實(shí)了產(chǎn)物與目標分子的結構相吻合。 |
| 關(guān)鍵詞：聚乙二醇; 氨基化; 蓋布瑞爾合成法; 合成 |
| 中圖分類(lèi)號：TQ325 文獻標識碼：A 文章編號：1009-9212(2006)01-0040-03 |
|
| 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 |
|
收稿日期：2005-09-08
|
| 閱讀全文 |
|