Cbz全保护RGD-OH的合成方法研究  

Research on synthetic methods of Cbz protected RGD-OH

作　　者：冯佳彩 齐国娣 刘毅[1] 杨毅华[1] 刘守信[1] 

机构地区：[1]河北科技大学化学与制药工程学院,河北石家庄050018

出　　处：《河北科技大学学报》2013年第5期430-433,共4页Journal of Hebei University of Science and Technology

基　　金：国家"973"计划前期研究专项课题(2011CB512007);河北省科技支撑计划(10276406D6)

摘　　要：采用碳端到氮端依次连接策略,以天冬氨酸、甘氨酸、精氨酸为起始原料,以HBTU为缩合剂,Asp(OBzl)-OAllyl顺次分别与Boc-甘氨酸和Cbz-Arg(Cbz)2偶联生成碳端和氮端保护的RGD。进一步在N-甲基吗啉存在下以Pd(PPh3)4催化脱去烯丙基,得到目标产物。中间产物和目标产物的分离、提纯采用重结晶和柱层析法,应用1 H NMR,13C NMR和MS等对其结构进行了表征。Followed the sequential strategy from C-terminal to N-terminal one by one,RGD with protected C-terminal and N-terminal are obtained by coupling reaction of Asp（OBzl）-OAllyl with Boc-Gly and Cbz-Arg（Cbz）2 respectively using Asp,Gly,Arg as raw materials and HBTU as coupling reagents.Allyl of the RGD derivatives is removed in the presence of（PPh3）4Pd/N-methylmorpholine to get the target product.The intermediates and the target product are purified by recrystallization and column chromatography,and their structures are determined by 1 H NMR,13 CNMR and MS.

关 键 词：HBTU Asp(OBzl)-OAllyl Boc-甘氨酸 Cbz-Arg(Cbz)2 偶联 RGD 

分 类 号：O629.72[理学—有机化学]