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)

1 LMC - Laboratoire de Marquage au Carbone 14
2 SCBM - Service de Chimie Bio-Organique et de Marquage
3 LCMCE - Laboratoire de Chimie Moléculaire et de Catalyse pour l'Energie (ex LCCEF)

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.

Domains: Chemical Sciences; Radiochemistry; Organic chemistry; Catalysis

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, 2019, 141 (2), pp.780-784. ⟨10.1021/jacs.8b12140⟩. ⟨cea-02420524⟩