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<p>The deuterium-labeled dabigatran etexilate and a series of <i>N</i>-(4-cyanophenyl)-1-(methyl-<i>d</i><sub>3</sub>)-5-carbamoyl-1<i>H</i>-benzo[<i>d</i>]imidazole-2-carbimidoyl chloride derivatives were prepared from commercially available 4-chloro-3-nitrobenzoate methyl ester as starting material and deuterium methylamine hydrochloride as the deuterium reagent. The structural properties of the intermediate derivatives were examined, and subsequently assessed for thrombin inhibition. The anticoagulant activity of the deuterium-labeled dabigatran etexilate was higher than that of unlabeled active ingredient, and most of these derivatives have certain valuable properties, which are expected to enrich the landscape of anticoagulant drug research.</p> Graphical abstract <p></p>

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Design, synthesis and anticoagulant activity evaluation of deuterium-labeled dabigatran etexilate and its intermediate derivatives

  • 期刊论文

  • 发表日期：

    2025年4月11日

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  • Dawei Liang,
  • Chang Wang,
  • Yuandong Ma,
  • Yueqiu Wang,
  • Luwen Zhang,
  • Jinhua Dong

摘要

The deuterium-labeled dabigatran etexilate and a series of N-(4-cyanophenyl)-1-(methyl-d3)-5-carbamoyl-1H-benzo[d]imidazole-2-carbimidoyl chloride derivatives were prepared from commercially available 4-chloro-3-nitrobenzoate methyl ester as starting material and deuterium methylamine hydrochloride as the deuterium reagent. The structural properties of the intermediate derivatives were examined, and subsequently assessed for thrombin inhibition. The anticoagulant activity of the deuterium-labeled dabigatran etexilate was higher than that of unlabeled active ingredient, and most of these derivatives have certain valuable properties, which are expected to enrich the landscape of anticoagulant drug research.

Graphical abstract