| 西曲瑞克的固相合成 |
| |
| 引用本文： | 石卫华,田素梅,项光亚,丁文锋,李振南,徐喆. 西曲瑞克的固相合成[J]. 中国药物化学杂志, 2010, 19(1): 40-43 |
| |
| 作者姓名： | 石卫华 田素梅 项光亚 丁文锋 李振南 徐喆 |
| |
| 作者单位： | 1.华中科技大学 同济药学院 药学系，湖北 武汉 430030；2. 深圳市康哲药业有限公司博士后工作站，广东 深圳 518057；3. 湖北武汉黄陂95942部队医院药房，湖北 武汉 430300；4. 湖北省天然药物与资源评价重点实验室，湖北 武汉 430030 |
| |
| 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化生产。
|
| 关 键 词： | 西曲瑞克；LH-RH受体阻断剂；Fmoc固相多肽合成 |
| 收稿时间： | 2009-05-11 |
| 修稿时间： | 2009-10-13 |
Solid phase synthesis of cetrorelix |
| |
| SHI Wei-hua,,TIAN Su-mei,,XIANG Guang-Ya,,DING Wen-feng,LI Zhen-nan,XU Zhe. Solid phase synthesis of cetrorelix[J]. Chinese Journal of Medicinal Chemistry, 2010, 19(1): 40-43 |
| |
| Authors: | SHI Wei-hua TIAN Su-mei XIANG Guang-Ya DING Wen-feng LI Zhen-nan XU Zhe |
| |
| Affiliation: | SHI Wei-hua1,2,TIAN Su-mei1,3,XIANG Guang-Ya1,4,DING Wen-feng2,LI Zhen-nan2,XU Zhe1(1.Pharmacy School of Tongji Medical College,Huazhong University of Science & Technology,Wuhan 430030,China,2.Work Station of Postdoctor,Shenzhen Kangzhe Pharmaceutical Company Limited,Shenzhen 518057,3.Drug Store,Huangpi 95942 Military Hospital,Wuhan 430300,4.Hubei Key Laboratory of Natural Medicinal Chemistry , Resource Evaluation,China) |
| |
| Abstract: | 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%. Conclusions The synthetic method of cetrorelix is brief, with higher purity and yield, and it is suitable to the industrial preparation of cetrorelix. |
| |
| Keywords: | cetrorelix LH-RH receptor antagonist Fmoc solid phase peptide synthesis |
| 本文献已被 CNKI 维普 等数据库收录！ |
| 点击此处可从《中国药物化学杂志》浏览原始摘要信息 |
|
点击此处可从《中国药物化学杂志》下载全文 |
|
