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Superacid-Mediated Late-Stage Aromatic Polydeuteration of Pharmaceuticals.
Appert, Emeline; Martin-Mingot, Agnès; Karam, Omar; Zunino, Fabien; Michelet, Bastien; Bouazza, Fodil; Thibaudeau, Sébastien.
Afiliación
  • Appert E; Superacid Group - Organic Synthesis Team, IC2MP, Université de Poitiers, UMR-CNRS 7285, 4 rue Michel Brunet, TSA 51106, 86073, Poitiers Cedex 9, France.
  • Martin-Mingot A; @rtMolecule, 1 rue Georges Bonnet, Bâtiment B37, 86000, Poitiers, France.
  • Karam O; Superacid Group - Organic Synthesis Team, IC2MP, Université de Poitiers, UMR-CNRS 7285, 4 rue Michel Brunet, TSA 51106, 86073, Poitiers Cedex 9, France.
  • Zunino F; @rtMolecule, 1 rue Georges Bonnet, Bâtiment B37, 86000, Poitiers, France.
  • Michelet B; @rtMolecule, 1 rue Georges Bonnet, Bâtiment B37, 86000, Poitiers, France.
  • Bouazza F; Superacid Group - Organic Synthesis Team, IC2MP, Université de Poitiers, UMR-CNRS 7285, 4 rue Michel Brunet, TSA 51106, 86073, Poitiers Cedex 9, France.
  • Thibaudeau S; @rtMolecule, 1 rue Georges Bonnet, Bâtiment B37, 86000, Poitiers, France.
Chemistry ; 28(49): e202201583, 2022 Sep 01.
Article en En | MEDLINE | ID: mdl-35689822
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. This study shows 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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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Hidrógeno Idioma: En Revista: Chemistry Asunto de la revista: QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Alemania
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Hidrógeno Idioma: En Revista: Chemistry Asunto de la revista: QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Alemania