2-(4-噻唑甲酰胺基)丙烯酰胺的合成  

Chemical Synthesis of 2-(4-Thiazole Formamide)Acrylamide

作　　者：魏雪娇[1] 刘晓会[1] 张魁礼 周伟[2] 周珮[2] WEI Xuejiao LIU Xiaohui ZHANG Kuili ZHOU Wei ZHOU Pei(College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201621）, China Department of Chemistry, Fudan University, Shanghai 200433, China)

机构地区：[1]上海工程技术大学化学化工学院,上海201620 [2]复旦大学化学系,上海200433

出　　处：《上海工程技术大学学报》2016年第3期214-217,共4页Journal of Shanghai University of Engineering Science

基　　金：上海工程技术大学大学生创新训练计划资助项目(cx1604004)

摘　　要：那西肽是含硫多肽类抗生素家族中的成员,具有多种药理活性.通过计算机辅助设计发现那西肽的边链:2-(4-噻唑甲酰胺基)丙烯酰胺是主要的活性中心.介绍了一种合成2-(4-噻唑甲酰胺基)丙烯酰胺的方法.以DL-丝氨酸为起始原料,经甲酯化、缩合、消除和氨解合成目标产物,收率分别达到97%、65%、70%和53%.该方法的建立为以后进行那西肽相关活性片段的结构修饰提供了原料合成方法.Nosiheptide is a member of the family of thiopeptide antibiotics,and has a special place for its biology and medicinal value.Based on computer aided design,it is found that nosiheptide side chain：2-（4-thiazole methanamide）acrylamide is the main active centers.Method for chemical synthesis of 2-（4-thiazole formamide）acrylamide was introduced.The target product 2-（4-thiazole formamide）acrylamide was obtained through reaction processes include esterification,condensation,elimination and aminolysis reaction with serine as the starting material,and which provides synthesis methods of raw materials for structural modification.

关 键 词：那西肽 2-(4-噻唑甲酰胺基)丙烯酰胺 合成 

分 类 号：O62[理学—有机化学]