Superacid-Mediated Late-Stage Aromatic Polydeuteration of Pharmaceuticals

Autor: Emeline Appert, Agnès Martin‐Mingot, Omar Karam, Fabien Zunino, Bastien Michelet, Fodil Bouazza, Sébastien Thibaudeau
Rok vydání: 2022
Předmět:
Zdroj: Chemistry (Weinheim an der Bergstrasse, Germany). 28(49)
ISSN: 1521-3765
Popis: 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.
Databáze: OpenAIRE