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

当前位置： X-MOL 学术 › ACS Comb. Sci. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Total Synthesis of Semaglutide Based on a Soluble Hydrophobic-Support-Assisted Liquid-Phase Synthetic Method
ACS Combinatorial Science Pub Date : 2020-10-15 , DOI: 10.1021/acscombsci.0c00134
Xingbang Liu ₁ , Na Zhang ₁ , Xiaotong Gu ₁ , Yinhui Qin ₁ , Di Song ₁ , Long Zhang ₁ , Shutao Ma ₁

Affiliation

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.

中文翻译：

基于可溶性疏水载体辅助液相合成法的索美鲁肽全合成

考虑到目前最有前景的降糖药物尤其是治疗2型糖尿病的索美鲁肽的生产成本高昂，具有优异收率和高纯度的索美鲁肽生产新合成路线至关重要。在此，我们报道了一种新开发的简单高效的索马鲁肽合成路线，基于可溶性疏水载体辅助液相合成方法，将Alloc-chemistry应用于索马鲁肽的主链肽和侧链肽的合成。 . 通过对反应条件的精心优化和合成后处理的创新策略，粗制司美鲁肽的总收率和纯度得到了令人满意的提高。

更新日期：2020-12-14

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南