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Article Dans Une Revue Chemistry - A European Journal Année : 2022

Superacid‐Mediated Late‐Stage Aromatic Polydeuteration of Pharmaceuticals

Résumé

The field of medicinal chemistry is currently witnessing a deuterium rush owing to the remarkable properties of this element as bioisoster of hydrogen atom. Aromatic hydrogen isotope exchange (HIE) is one of the most studied strategies nowadays as it promises to access deuterium-modified drugs directly from their non-labeled parents. While most of the recent studies focus on metal-catalyzed C–H activation strategy, the use of superacidic conditions has been largely overlooked. Here, we show that the use of TfOD as reaction medium allows the late-stage polydeuteration of a broad library of pharmaceuticals bearing a wide array of functional groups, complementing existing procedures.
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Dates et versions

hal-03769665 , version 1 (05-09-2022)

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Emeline Appert, Agnès Martin-Mingot, Omar Karam, Fabien Zunino, Bastien Michelet, et al.. Superacid‐Mediated Late‐Stage Aromatic Polydeuteration of Pharmaceuticals. Chemistry - A European Journal, 2022, 28 (49), pp.e202201583. ⟨10.1002/chem.202201583⟩. ⟨hal-03769665⟩
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