聚[α,β-(N-2-乙羟基)-DL-天冬酰胺]-美他沙酮前药的合成与表征  

Synthesis and characterization of poly-α,β-(2-hydroxyethyl) DL-asparamid-metaxalone prodrug

作　　者：高丽娟[1] 张娟[1] 刘毅锋[1] 乔长安 周永柱[1] 

机构地区：[1]西北大学应用化学研究所,陕西西安710069 [2]陕西出入境检验检疫局,陕西西安710068

出　　处：《西北大学学报（自然科学版）》2009年第6期989-991,共3页Journal of Northwest University（Natural Science Edition）

基　　金：陕西省教育厅专项基金资助项目(09JK791)

摘　　要：目的研究聚[α,β-(N-2-羟乙基)-DL-天冬酰胺]-美他沙酮前药的合成方法。方法采用氯乙酰氯作为连接基试剂和美他沙酮的N1反应,生成中间体N-氯乙酰基美他沙酮,中间体再与聚[α,β-(N-2-羟乙基)-DL-天冬酰胺]反应,合成了目标产物,并利用红外、DSC对其进行分析和表征。结果美他沙酮在目标产物中的质量分数可以达到16.1%。结论该方法操作简单,反应条件温和,具有良好的应用前景。Aim To report a method for synthesis of poly-α ,β-（2-hydroxyethyl）-DL-asparamid-metaxalone （PHEA-Met） prodrug. Methods The prodrug was synthesized by two steps： （1） the intermediate N-Acetyl chloride metaxalonethe is prepared by linking the choroacetic chloride to the metaxalone; （2） The target compound PHEA-Met was synthesized from PHEA and intermediate. It was characterized by IR and DSC. Results The contents of metaxalone in prodrug was more than 16. 1%. Conclusion The method of preparation of the prodrug is simple and usable with mild condition, which has wide application prospect.

关 键 词：聚[Ot 卢一(N一2一羟乙基)一DL一天冬酰胺] 美他沙酮 合成 前药 

分 类 号：O621.3[理学—有机化学]