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<p>Labelled compounds bearing hydrogen isotopes are keystones in diverse areas constituting a multi-billion dollar global market including drugs, diagnostics, biology, toxicology and smart materials. While hydrogen deuterium exchange (HDE) methods hold promise as relevant tools for the late-stage and one-step preparation of deuterium-labelled compounds, they often fall short in achieving sufficient isotopic purity combined either with a site-selectivity or with a full deuteration process, highlighting the need for further development and optimisation. This report pinpoints an approach to unlock the potential of HDE using the concept of iterative runs in continuous-flow technology (recirculation process). This closed-loop process grants access now to deuterated compounds with high isotopic purities, labelled at a precise site or perdeuterated on demand, in a fast, productive, and environmentally friendly way.</p>

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Unlocking the potential of hydrogen deuterium exchange via an iterative continuous-flow deuteration process

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年2月3日

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  • Kevin Tatoueix,
  • Marco Lepron,
  • Cédric Barboux,
  • Marie-Christine Scherrmann,
  • Grégory Pieters,
  • Sophie Feuillastre

摘要

Labelled compounds bearing hydrogen isotopes are keystones in diverse areas constituting a multi-billion dollar global market including drugs, diagnostics, biology, toxicology and smart materials. While hydrogen deuterium exchange (HDE) methods hold promise as relevant tools for the late-stage and one-step preparation of deuterium-labelled compounds, they often fall short in achieving sufficient isotopic purity combined either with a site-selectivity or with a full deuteration process, highlighting the need for further development and optimisation. This report pinpoints an approach to unlock the potential of HDE using the concept of iterative runs in continuous-flow technology (recirculation process). This closed-loop process grants access now to deuterated compounds with high isotopic purities, labelled at a precise site or perdeuterated on demand, in a fast, productive, and environmentally friendly way.