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简单、可扩展的流动相肽键溶液相合成。

Straightforward, scalable, solution-phase synthesis of peptide bonds in flow.

作者信息

Wilson Zoe E, Lopez Enol, Flodén Nils J, Watkins Charis, Bianchini Giulia, Ley Steven V

机构信息

Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW UK.

School of Chemical Sciences, University of Auckland, Auckland, New Zealand.

出版信息

J Flow Chem. 2025;15(2):67-77. doi: 10.1007/s41981-025-00347-2. Epub 2025 Mar 12.

Abstract

UNLABELLED

We report the development of simple solution-phase flow conditions for the scalable synthesis of peptides using in-situ activation as mixed anhydrides, contributing to the synthetic toolbox of available solution-phase flow reactions. This approach has been used for the preparation of a series of diverse dipeptides in plug flow, and then continuous flow conditions (< 10 mmol) were developed and applied to the gram scale synthesis of the hexapeptide linear precursor for the bioactive cyclic peptide segetalin A as further proof of the utility of this approach.

SUPPLEMENTARY INFORMATION

The online version contains supplementary material available at 10.1007/s41981-025-00347-2.

摘要

未标注

我们报告了一种简单的溶液相流动条件的开发,该条件用于通过原位活化作为混合酸酐来可扩展地合成肽,为可用的溶液相流动反应的合成工具箱做出了贡献。这种方法已用于在活塞流中制备一系列不同的二肽,然后开发了连续流动条件(<10 mmol)并将其应用于生物活性环肽segetalin A的六肽线性前体的克级合成,以进一步证明该方法的实用性。

补充信息

在线版本包含可在10.1007/s41981-025-00347-2获取的补充材料。

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