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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。
Objective To optimize the solid-phase synthesis conditions and purification methods of cetrorelix. Methods Fmoc solid phase synthesis method was used, and Rink Amide-AM Resin was used as the solid phase carrier. DIC / HOBt or DIC / HOAt was used as the condensing agent and purified by preparative reversed-phase high performance liquid chromatography. Results Crude peptides of Cetrorelix were synthesized. The purity of the crude product was 94.8%. The crude peptide was purified by preparative reversed-phase high performance liquid chromatography (HPLC). The purity of the purified peptide was 99%. The total yield was 62%. Conclusion The synthesis method is simple and easy, the product purity and yield are very high, suitable for the industrial production of Cirrus.