Cbz全保护RGD-OH的合成方法研究

Research on synthetic methods of Cbz protected RGD-OH

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.