酰氯法制备布洛芬-聚乙二醇酯  

Synthesis and Characterization of Ibuprofen-Polyethylene Glycol Ester wth New Methods

作　　者：宋春梅[1] 张亮[1] 庄小璐[1] 周卫青[1] 常飞[1] 

机构地区：[1]华东师范大学化学系,上海200062

出　　处：《高分子材料科学与工程》2011年第7期140-142,共3页Polymer Materials Science & Engineering

基　　金：上海市经委项目(48100270)

摘　　要：分别用氯化亚砜(方法1)、草酰氯(方法2)两种方法将布洛芬[2-(4-异丁基苯基)丙酸]活化成2-(4-异丁基苯基)丙酰氯(Ⅰ),再与聚乙二醇(PEG)的端羟基反应生成PEG修饰的布洛芬-聚乙二醇酯,即2-(4-异丁基苯基)丙酸-聚乙二醇酯(Ⅱ)。分别用核磁共振(1H-NMR)、红外光谱(IR)和凝胶渗透色谱(GPC)对其进行了表征,结果表明成功合成了含布洛芬端基的PEG大单体,分子量分布窄,d为1.047。溶解性试验表明Ⅱ的水溶性很好。草酰氯法反应条件温和,产率更高,说明草酰氯法更优。Ibuprofen-polyethylene glycol ester（Ⅱ）,2-（4-isobutylphenyl） propionic acid-polyethylene glycol ester,could be designed and obtained from the reaction of polyethylene glycol（PEG） with 2-（4-isobutylphenyl） propionic acyl chloride（Ⅰ）,which was prepared in high yield by the reaction of ibuprofen with thionyl chloride（method 1） or oxalyl chloride（method 2）.The structure analysis and characterization of Ⅱ were studied by 1H nuclear magnetic resonance spectrum（1H-NMR）,infrared spectrum（IR） and gel permeation in chromatography（GPC） method.The results show that Ⅱ is synthesized successfully,and the molecule distribution of Ⅱ is 1.047.Ⅱ is dissolvable in most organic solvents such as CH2Cl2,CHCl3,THF,DMF and DMSO.The solubility of Ⅱ has been improved in aqueous solutions.Compared with method 1,the method 2 has the advantages of milder reaction condition,higher yield.

关 键 词：布洛芬 聚乙二醇 酰氯 高分子药物 

分 类 号：TQ460.3[化学工程—制药化工]