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Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO₂

Author:
Destro, Gianluca, Loreau, Olivier, Marcon, Elodie, Taran, Frédéric, Cantat, Thibault, Audisio, Davide
Source:
Journal of the American Chemical Society 2018 v.141 no.2 pp. 780-784
ISSN:
1520-5126
Subject:
carbon, carbon dioxide, carboxylic acids, drugs, radioactive waste, radionuclides
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.
Agid:
6271651