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Updated: Nov 9, 2025

Enhancing Efficiency and Radiolabeling Yields of Carbon-11 Radioligands for Clinical Research Using the Loop Method
Published on: December 20, 2024
Direct Carbon Isotope Exchange of Pharmaceuticals via Reversible Decyanation
Minghao Feng1, Joao De Oliveira1,2, Antoine Sallustrau1
1Université Paris Saclay, CEA, DMTS, Service de Chimie Bio-organique et Marquage, 91191 Gif-sur-Yvette, France.
Abstract:
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. By utilizing the radiolabeled precursor Zn([14C]CN)2, this protocol allows the insertion of the desired carbon tag without the need for structural modifications, in a single step. By 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.
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