一种索玛鲁肽的制备方法

文档序号:23725 发布日期:2021-09-21 浏览:26次 >En<

阅读说明:本技术 一种索玛鲁肽的制备方法 (Preparation method of somaglutide ) 是由 李新宇 付玉清 张利香 姚林 李文静 于 2020-07-09 设计创作,主要内容包括:一种索玛鲁肽的制备方法,该方法包括:通过固相合成得到索玛鲁肽树脂,经裂解,脱保护,得到索玛鲁肽粗肽,纯化、冻干后得到索玛鲁肽精肽,其中包括固相合成索玛鲁肽1-6肽片段树脂,经裂解和纯化作为第一个肽片段;合成索玛鲁肽20位带侧链基团的赖氨酸,作为第二个肽片段。在该方法中,制备索玛鲁肽1-6位全保护肽片段,将其作为关键起始物料应用于索玛鲁肽固相合成中,降低了D-His、D-Glu、D-Thr、D-Phe消旋杂质和+Gly杂质的产生,降低了粗品纯化的难度,提高了索玛鲁肽的纯度和收率,降低了合成成本,有利于工业化大生产。(A method of preparing somaglutide, the method comprising: obtaining a soxhlet peptide resin through solid phase synthesis, obtaining a crude soxhlet peptide through cracking and deprotection, obtaining a fine soxhlet peptide through purification and freeze-drying, wherein the fine soxhlet peptide comprises a first peptide fragment which is obtained by solid phase synthesis of the soxhlet peptide 1-6 peptide fragment resin and is obtained through cracking and purification; and synthesizing the lysine with a side chain group at the 20 th position of the somaglutide as a second peptide fragment. In the method, the 1-6 position total-protection peptide fragment of the somaglutide is prepared and is used as a key starting material for solid-phase synthesis of the somaglutide, so that the generation of D-His, D-Glu, D-Thr, D-Phe racemization impurities and &#43; Gly impurities is reduced, the difficulty of crude product purification is reduced, the purity and yield of the somaglutide are improved, the synthesis cost is reduced, and the industrial mass production is facilitated.)

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