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Direct Carbon Isotope Exchange of Pharmaceuticals via Reversible Decyanation
preprintsubmitted on 17.02.2021, 23:26 and posted on 18.02.2021, 13:23 by Minghao Feng, Joao De Oliveira, Antoine Sallustrau, Gianluca Destro, Pierre Thuéry, Sebastien Roy, Thibault Cantat, Charles S. Elmore, Jörg Blankenstein, Frédéric Taran, Davide Audisio
The incorporation of carbon-14 allows tracking of organic molecules and provides vital knowledge on their fate. This information is critical in pharmaceutical development, crop science and human food safety evaluation. Herein, a transition-metal-catalyzed procedure enabling carbon isotope exchange on aromatic nitriles is described. Utilizing the radiolabeled precursor Zn([14C]CN)2, this protocol allows the insertion of the desired carbon tag without need of structural modifications, in a single step. Reducing synthetic costs and limiting the generation of radioactive waste, this procedure will facilitate the labeling of nitrile containing drugs and accelerate 14C-based ADME studies supporting drug development.