脂质体药用辅料mPEG2000-DSPE的合成  

Synthesis of Pharmaceutical Excipients of Liposomesm PEG2000-DSPE

作　　者：苏长会 朱瑶怡 丁志远 闫荣杰 刘霞[2] SU Chang-hui;ZHU Yao-yi;DING Zhi-yuan;YAN Rong-jie;LIU Xia(School of Chemistry and Life Science,Nanjing University Jinling College,Nanjing 210089,China;College of Environment Science and Ecology,Jiangsu Open University,Nanjing 210036,China)

机构地区：[1]南京大学金陵学院化学与生命科学学院,江苏南京210089 [2]江苏开放大学环境与生态学院,江苏南京210036

出　　处：《合成化学》2019年第12期982-984,995,共4页Chinese Journal of Synthetic Chemistry

基　　金：江苏省高校自然科学基金资助项目(16KJB150007);江苏省大学生创新基金资助项目(201813646019Z)

摘　　要：以氧氯化磷、乙醇胺及1,2-二硬脂酸甘油酯为原料,经环合、磷酰化及水解反应制得1,2-二硬脂酰甘油磷酰乙醇胺(DSPE);在N,N′-羰基二咪唑作用下,DSPE与甲氧基聚乙二醇(mPEG2000)反应合成了1,2-二硬脂酰甘油磷脂酰乙醇胺-N-甲氧基聚乙二醇2000(mPEG2000-DSPE),其结构经1 H NMR,IR和MS(ESI)确证。1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine(DSPE)was prepared by the reaction of cyclization,phosphorylation and hydrolysis reaction from glycerol-1,2-distearate,phosphorusoxychloride and 2-aminoethanol.Then,DSPE was coupled with mPEG2000 under the action of N,N′-carbonyldiimidazole(CDI)to synthesis mPEG2000-DSPE.The structure was confirmed by 1 H NMR,IR and MS(ESI).

关 键 词：聚乙二醇 脂质体 磷脂 N N′-羰基二咪唑 磷酰乙醇胺 合成 

分 类 号：O623.7[理学—有机化学]