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Journal Articles Journal of the American Chemical Society Year : 2019

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

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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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Dates and versions

cea-02420524 , version 1 (20-12-2019)

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