阿昔洛韦衍生物SACV-Gln-Gln的合成及其表征  

Synthesis and characterization of acyclovir derivative SACV-Gln-Gln

作　　者：刘捷[1] 穆冰彦[1] 马丽[1] 赵东欣[1] 卢奎[1] 

机构地区：[1]河南工业大学化学化工学院,河南郑州450001

出　　处：《河南工程学院学报（自然科学版）》2013年第1期25-27,共3页Journal of Henan University of Engineering：Natural Science Edition

基　　金：国家自然科学基金(20772023)

摘　　要：采用Fmoc固相合成法制备了阿昔洛韦衍生物———琥珀酰阿昔洛韦-谷氨酰胺酰谷氨酰胺(SACV-Gln-Gln),经过二肽修饰后的阿昔洛韦水溶性显著提高.合成过程如下:以阿昔洛韦与琥珀酸酐为原料,在三乙胺碱性条件下合成了琥珀酰阿昔洛韦[9-(2-丁二酸单酰乙氧基甲基)鸟嘌呤](SACV),然后采用Fmoc固相合成法合成了一个新的阿昔洛韦衍生物SACV-Gln-Gln,产率为76%,利用1H NMR和ESI-MS对其结构进行了表征.In this paper a new acyclovir dipeptide derivative, SACV-Gln-Gln was synthesized by Fmoc solid synthesis method. Succinyl acyelovir （SACV） was prepared by acyclovir which was coupled with succinic anhydride in the present of triethylamine. The yield of SACV-Gln-Gln was about 76%. The hydrophilic properties of SACV-Gln-Gln was significantly enhanced, compared with acyclovir. The structures of SACV and SACV-Gln-Gln were characterized by l H NMR and ESI - MS.

关 键 词：阿昔洛韦 琥珀酰阿昔洛韦 固相合成法 二肽 

分 类 号：O623[理学—有机化学]