西曲瑞克的固相合成  

Solid phase synthesis of cetrorelix

作　　者：石卫华[1,2] 田素梅[1,3] 项光亚[1,4] 丁文锋 李振南 徐喆[1] 

机构地区：[1]华中科技大学同济药学院药学系 [2]深圳市康哲药业有限公司博士后工作站 [3]湖北武汉黄陂95942部队医院药房 [4]湖北省天然药物与资源评价重点实验室

出　　处：《中国药物化学杂志》2010年第1期40-43,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的优化西曲瑞克的固相合成条件及纯化方法。方法采用Fmoc固相合成法,以Rink Amide-AM Resin为固相载体,以DIC/HOBt或DIC/HOAt为缩合剂,采用制备型反相高效液相色谱法进行纯化。结果合成西曲瑞克粗肽,粗品纯度为94.8%;粗肽经制备型反相高效液相色谱纯化,所得精肽的纯度高达99%,总收率为62%。结论该合成方法简单易行,产品纯度及收率都很高,适合用于西曲瑞克的工业生产。Aim To optimize the solid phase synthesis method of cetrorelix and its purification. Methods Cetrorelix was synthesized by Fmoc solid phase peptide synthesis methods via Rink Amide-AM Resin, using HOBt/DIC or HOAt/DIC as activation system, and was purified by preparative HPLC. Results The purity of the crude peptide was 94.8 %. The purity of cetrorelix can be increased to more than 99 % through preparative HPLC, and the overall yield was about 62%. Conclusion The synthetic method of cetrorelix is brief with higher purity and yield, and it is suitable to the industrial preparation of cetrorelix.

关 键 词：西曲瑞克 LH-RH受体阻断剂 Fmoc固相多肽合成 

分 类 号：R914[医药卫生—药物化学]