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([ 14 C]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 14 C-based ADME studies supporting drug development. File list (2) download file view on ChemRxiv Manuscript.pdf (1.47 MiB) download file view on ChemRxiv Supporting Information.pdf (9.86 MiB)
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([<sup>14</sup>C]CN)<sub>2</sub>,
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 <sup>14</sup>C-based
ADME studies supporting drug development.
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([<sup>14</sup>C]CN)<sub>2</sub>,
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 <sup>14</sup>C-based
ADME studies supporting drug development.
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