One‐Pot Synthesis of (11)C‐Labelled Primary Benzamides via Intermediate [(11)C]Aroyl Dimethylaminopyridinium Salts

Electrophilic (11)C‐labelled aroyl dimethylaminopyridinium salts, obtained by carbonylative cross‐coupling of aryl halides with [(11)C]carbon monoxide, were prepared for the first time and shown to be valuable intermediates in the synthesis of primary [(11)C]benzamides. The methodology furnished a s...

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Detalles Bibliográficos
Autores principales: Ferrat, Mélodie, Dahl, Kenneth, Schou, Magnus
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2021
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8251633/
https://www.ncbi.nlm.nih.gov/pubmed/33885193
http://dx.doi.org/10.1002/chem.202100544
Descripción
Sumario:Electrophilic (11)C‐labelled aroyl dimethylaminopyridinium salts, obtained by carbonylative cross‐coupling of aryl halides with [(11)C]carbon monoxide, were prepared for the first time and shown to be valuable intermediates in the synthesis of primary [(11)C]benzamides. The methodology furnished a set of benzamide model compounds, including the two poly (ADP‐ribose) polymerase (PARP) inhibitors niraparib and veliparib, in moderate to excellent radiochemical yields. In addition to providing a convenient and practical route to primary [(11)C]benzamides, the current method paves the way for future application of [(11)C]aroyl dimethylaminopyridinium halide salts in positron emission tomography (PET) tracer synthesis.

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