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. 2019 Jan 16;141(2):780-784.
doi: 10.1021/jacs.8b12140. Epub 2018 Dec 31.

Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO2

Gianluca Destro  1 , Olivier Loreau  1 , Elodie Marcon  1 , Frédéric Taran  1 , Thibault Cantat  2 , Davide Audisio  1
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Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO2

Gianluca Destro et al. J Am Chem Soc. .

Abstract

A copper-catalyzed procedure enabling dynamic carbon isotope exchange is described. Utilizing the universal precursor [14C]CO2, 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 14C-based ADME studies supporting drug development.

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