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4-Nitrophenyl activated esters are superior synthons for indirect radiofluorination of biomolecules

Indirect radiolabelling has for a long time been the mainstay strategy for radiofluorination of biomolecules. Acylation of biomolecules through the use of an (18)F-labelled activated ester is a standard method for indirect radiolabelling. However, the preparation of (18)F-labelled activated esters i...

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Detalles Bibliográficos
Autores principales: Haskali, Mohammad B., Farnsworth, Ashleigh L., Roselt, Peter D., Hutton, Craig A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7517343/
https://www.ncbi.nlm.nih.gov/pubmed/33479687
http://dx.doi.org/10.1039/d0md00140f
Descripción
Sumario:Indirect radiolabelling has for a long time been the mainstay strategy for radiofluorination of biomolecules. Acylation of biomolecules through the use of an (18)F-labelled activated ester is a standard method for indirect radiolabelling. However, the preparation of (18)F-labelled activated esters is typically a complex and multistep procedure. Herein, we describe the use of 4-nitrophenyl (PNP) activated esters to rapidly prepare (18)F-labelled acylation synthons in one step. Furthermore, we present a comparative study of PNP activated esters and the commonly utilised 2,3,5,6-tetrafluorphenyl (TFP) activated esters under direct radiofluorination conditions and demonstrate their relative acylation behaviour. We demonstrate the superiority of PNP esters under direct radiofluorination conditions with favourable acylation kinetics.