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Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO$_2$

Gianluca Destro 1, 2 Olivier Loreau 2 Elodie Marcon 2 Frédéric Taran 1, 2 Thibault Cantat 3, * Davide Audisio 2, *
* Corresponding author
1 LMC - Laboratoire de Marquage au Carbone 14
SCBM - Service de Chimie Bio-Organique et de Marquage : DRF/JOLIOT
3 LCMCE - Laboratoire de Chimie Moléculaire et de Catalyse pour l'Energie (ex LCCEF)
NIMBE UMR 3685 - Nanosciences et Innovation pour les Matériaux, la Biomédecine et l'Energie (ex SIS2M)
Abstract : A copper-catalyzed procedure enabling dynamic carbon isotope exchange is described. Utilizing the universal precursor [$^{14}$C]CO$_2$ , this protocol allows to insert, in one single step, the desired carbon tag into carboxylic acids with no need of structural modifications. Reducing synthetic costs and limiting the generation of radioactive waste, this procedure will facilitate the access to carboxylic acids containing drugs and accelerate early $^{14}$C-based ADME studies supporting drug development.
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Submitted on : Friday, December 20, 2019 - 12:09:04 AM
Last modification on : Wednesday, July 8, 2020 - 3:37:46 AM
Long-term archiving on: : Saturday, March 21, 2020 - 1:12:19 PM

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Gianluca Destro, Olivier Loreau, Elodie Marcon, Frédéric Taran, Thibault Cantat, et al.. Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO$_2$. Journal of the American Chemical Society, American Chemical Society, 2019, 141 (2), pp.780-784. ⟨10.1021/jacs.8b12140⟩. ⟨cea-02420524⟩

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