甲磺酸加贝酯的合成工艺改进  

Improved synthesis of gabexate mesylate

作　　者：姚金烽[1] 杨文革[1] 沈磊[1] 赵晓磊[1] 陆修涛[1] 胡永红[1] 

机构地区：[1]南京工业大学药学院,江苏南京210009

出　　处：《化学试剂》2010年第5期473-474,共2页Chemical Reagents

基　　金：江苏省科技厅资助项目(BE2008399)

摘　　要：以己内酰胺为原料经水解得氨基己酸,然后与S-甲基异硫脲硫酸盐反应得胍基己酸,经盐酸化得中间体胍基己酸盐酸盐,再经酯缩合,两步酸化得标题化合物。改进后的工艺原料廉价易得,反应条件温和,操作简单。总收率65%。Gabexate mesylate was synthesized from caprolactam by hydrolysis to give 6-aminohexanoic acid,which was subjected to reaction with S-methylisothioureasulfate to obtain 6-guandinyl hexanoic acid,followed by esterification and two steps of acidification,resulting in an overall product yield of 65%.The improved process has the advantages of cheap raw materials used,mild reaction conditions and simple operation.

关 键 词：甲磺酸加贝酯 己内酰胺 工艺优化 

分 类 号：O626.2[理学—有机化学]