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Intercambio dinámico de isótopos de carbono de productos farmacéuticos con etiqueta CO2
Gianluca Destro1, Olivier Loreau1, Elodie Marcon1
1Service de Chimie Bio-organique et Marquage (SCBM), CEA/DRF/JOLIOT, Université Paris Saclay , F-91191 Gif-sur-Yvette , France.
Journal of the American Chemical Society
|December 27, 2018
Resumen
Este estudio introduce un nuevo método catalizado por cobre para el intercambio dinámico de isótopos de carbono utilizando CO2. Esto simplifica el etiquetado de ácidos carboxílicos, reduciendo los costos y el desperdicio para los estudios de desarrollo de fármacos.
Área de la Ciencia:
- Química orgánica
- La radioquímica
- Química medicinal
Sus antecedentes:
- Los ácidos carboxílicos son cruciales en el desarrollo de fármacos.
- El etiquetado radiactivo es esencial para los estudios ADME.
- Los métodos actuales para el etiquetado C pueden ser complejos y costosos.
Objetivo del estudio:
- Desarrollar un método simplificado para la introducción de isótopos de carbono en ácidos carboxílicos.
- Para permitir un etiquetado C eficiente utilizando un precursor universal.
- Reducir los costes sintéticos y los residuos radiactivos en el desarrollo de fármacos.
Principales métodos:
- Una nueva reacción de intercambio dinámico de isótopos de carbono catalizada por el cobre.
- Utilizando el dióxido de carbono (CO2) como el precursor universal.
- Etiquetado isotópico directo de un solo paso de ácidos carboxílicos sin modificación estructural.
Principales resultados:
- Implementación exitosa de un procedimiento catalizado por el cobre para el intercambio dinámico de isótopos de carbono.
- La inserción eficiente y directa de C en los ácidos carboxílicos.
- Reducción demostrada de los costes sintéticos y de la generación de residuos radiactivos.
Conclusiones:
- El protocolo descrito facilita el acceso a los ácidos carboxílicos etiquetados con C.
- Este método acelera los primeros estudios de ADME basados en C.
- El procedimiento apoya el desarrollo de fármacos simplificando el etiquetado radioactivo.
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