西仑吉肽的固相合成  

Solid phase synthesis of cilengitide

作　　者：张波[1] 王卫国[2] 康武[1] 智小霞[1] 姚忠[1] 徐红岩[2] 

机构地区：[1]南京工业大学制药与生命科学学院,江苏南京210009 [2]中国科学院上海有机化学研究所,上海200032

出　　处：《化学试剂》2012年第11期1041-1042,1046,共3页Chemical Reagents

摘　　要：采用Fmoc固相合成法,选用2-氯三苯甲基氯树脂作为固相载,HBTU/HOBt和HATU/HOBt为缩合剂,合成全保护线性肽。以V(DCM)∶V(THF)=1∶1为溶剂,HATU/HOBt为缩合剂,合成全保护环肽。最后脱除保护基得终产物西仑吉肽。Fully-protected linear peptide was synthesized by Fmoc solid phase peptide synthesis methods. The solid phase carrier was 2-chlorotrityl chloride resin. HATU/HOBt and HBTU/HOBt were used as the coupling reagents. The synthe- sis of fully-protected cyclic peptide used THF/DCM （ at a ra- tio of 1：1 by volume） as the solvent and HATU/HOBt as the coupling reagents. Finally cilengitide could be obtained by deprotection reaction.

关 键 词：固相多肽合成 环肽 2-氯三苯甲基氯树脂 西仑吉肽 

分 类 号：O629.72[理学—有机化学]