Direct Carbon Isotope Exchange of Pharmaceuticals via Reversible Decyanation.
J Am Chem Soc
; 143(15): 5659-5665, 2021 04 21.
Article
em En
| MEDLINE
| ID: mdl-33825486
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Preparações Farmacêuticas
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article