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<p>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 (&lt; 10&#xa0;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.</p> Graphical Abstract <p></p>

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

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年3月12日

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

摘要

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.

Graphical Abstract