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.
出处
《西北大学学报（自然科学版）》
CAS
CSCD
北大核心
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)
