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.
出处
《中国药物化学杂志》
CAS
CSCD
2010年第1期40-43,共4页
Chinese Journal of Medicinal Chemistry
