一种去除接枝胆固醇的两亲性高分子材料中DMAP中间体的方法

A novel method for removing DMAP intermediate from cholesterol-coupled amphiphilic polymers

目的以泊洛沙姆188-胆固醇碳酸酯为例,探寻去除接枝胆固醇的两亲性高分子材料中4-二甲氨基吡啶(4-dimethylaminopyridine,DMAP)中间体的最优方法。方法以DMAP中间体残余百分率为评价指标,考察酸洗-饱和Na Cl洗-水洗法、阳离子交换树脂法、透析冻干法及甲苯沉淀法对泊洛沙姆188-胆固醇碳酸酯的纯化效率。结果上述四种方法中,甲苯沉淀法的DMAP中间体残余百分率最低,接近于0。结论通过与酸洗-饱和Na Cl洗-水洗法、阳离子交换树脂法及透析冻干法进行对比,证明了甲苯沉淀法在此合成中的简便性和高效性,为接枝胆固醇的两亲性高分子材料中DMAP的去除提供了参考。

Objective To optimize the process of removing DMAP intermediate from cholesterol-coupled amphiphilic polymers for the example of P188-CHMC. Methods Taking residual rate of DMAP intermediate as the assessment index,four methods including HCl-saturated Na Cl-H2 O,cation resin column,dialysis and lyophilization and deposition ith toluene ere used to purify DMAP intermediate in order to investigate the purification efficiency. Results In the above methods,the DMAP intermediate could be completely removed by deposition ith toluene method. Conclusions Compared ith other three methods,deposition ith toluene method is considered as the most simple and efficient ay to remove DMAP intermediate,which providing a reference for the purification of cholesterol-coupled amphiphilic polymers.