混合酸酐法合成内吗啡肽-1  

Synthesis of endomorphin-1 with mixed anhydride method

作　　者：梁月洁[1] 孟庆国[1] 孙海军[1] 毛杨[1] 张江峰[1] 

机构地区：[1]山东烟台大学药学院,烟台264005

出　　处：《中国新药杂志》2008年第16期1405-1407,共3页Chinese Journal of New Drugs

摘　　要：目的:采用液相方法合成内吗啡肽-1。方法:以混合酸酐法先分别合成N端二肽片段和C端二肽片段,再缩合得到四肽,以50%TFA/DCM(三氟乙酸/二氯甲烷)脱除N端Boc(叔丁氧羰基)保护基。结果:合成的内吗啡肽-1(EM-1),收率较文献高,结构经质谱和1H NMR确证。结论:混合酸酐法操作简便,反应时间缩短,副产物少,易分离纯化,适用于大量制备。Objective： To synthesize endomorphin-1 with liquid phase condensation. Methods： N-terminal dipeptide and C-terminal dipeptide have been synthesized respectively using the mixed anhydride method, and coupled ; finally the pure EM-1 was obtained. Results ： Endomorphin-1 （ EM-1 ） was successfully synthesized, and was conformed by ESI-MS and ^1H NMR. Conclusion： The shorter reaction time and higher yield than those reported mixed anhydride method is conveniently performed with in literature, and can be used in large scale preparation.

关 键 词：内吗啡肽-1 混合酸酐法 合成 

分 类 号：R971.1[医药卫生—药品]