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以Rink Amide MBHA树脂为载体,Fmoc保护的氨基酸为原料,HOBt、DIC为缩合试剂,按照加尼瑞克的氨基酸序列进行固相合成得到加尼瑞克粗肽;经2步反相高效液相色谱法进行分离纯化,得到纯度大于99%的加尼瑞克纯品,总收率达31.03%;最后对产品中的醋酸含量进行控制,经过冻干得到了纯度大于99%的醋酸加尼瑞克样品;讨论了醋酸加尼瑞克制备工艺过程中的关键因素,并对工艺条件进行了优化。
Using Rink Amide MBHA resin as carrier, Fmoc-protected amino acids as raw materials, HOBt and DIC as condensation reagents, solid-phase synthesis of ganirelix was performed according to the amino acid sequence of ganirelix. Chromatographic separation and purification to obtain pure purity of greater than 99% Gannelic pure product, the total yield was 31.03%; finally the content of acetic acid in the product was controlled by lyophilization to obtain a purity of greater than 99% G samples; the key factors in the process of preparation of Gannellacetate were discussed, and the process conditions were optimized.