【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.更多还原

【Abstract】 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.更多还原