Total Synthesis of Semaglutide Based on a Soluble Hydrophobic-Support-Assisted Liquid-Phase Synthetic Method

IF 4.3 3区 材料科学 Q1 ENGINEERING, ELECTRICAL & ELECTRONIC
Xingbang Liu, Na Zhang, Xiaotong Gu, Yinhui Qin, Di Song, Long Zhang, Shutao Ma*
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引用次数: 5

Abstract

Considering the high cost of the production of semaglutide, which is currently the most promising antidiabetic drug especially for the treatment of type 2 diabetes mellitus, a new synthetic route of semaglutide production that possesses excellent yield and high purity is of vital importance. Herein, we reported a newly developed synthetic route of semaglutide that is simple and efficient, based on a soluble hydrophobic-support-assisted liquid-phase synthetic method by applying Alloc-chemistry to the synthesis of the main chain peptide and side chain peptide of semaglutide. With careful optimization of the reaction conditions and innovative strategy of post-synthetic treatments, the total yield and purity of the crude semaglutide was improved satisfactorily.

Abstract Image

基于可溶疏水载体辅助液相法的半马鲁肽全合成
semaglutide是目前最有前途的抗糖尿病药物,尤其是治疗2型糖尿病的药物,鉴于其生产成本高,寻找一种收率高、纯度高的合成途径至关重要。本文报道了一种基于水溶性疏水载体辅助液相合成方法,利用alloc化学方法合成了半马鲁肽的主链肽和侧链肽的新方法,该方法简单高效。通过对反应条件的优化和合成后处理策略的创新,使粗产物的总收率和纯度得到了满意的提高。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
7.20
自引率
4.30%
发文量
567
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