4-Nitrophenyl activated esters are superior synthons for indirect radiofluorination of biomolecules
AuthorHaskali, MB; Farnsworth, AL; Roselt, PD; Hutton, CA
Source TitleRSC Medicinal Chemistry
PublisherROYAL SOC CHEMISTRY
AffiliationSchool of Chemistry
Sir Peter MacCallum Department of Oncology
Document TypeJournal Article
CitationsHaskali, M. B., Farnsworth, A. L., Roselt, P. D. & Hutton, C. A. (2020). 4-Nitrophenyl activated esters are superior synthons for indirect radiofluorination of biomolecules. RSC MEDICINAL CHEMISTRY, 11 (8), pp.919-922. https://doi.org/10.1039/d0md00140f.
Access StatusOpen Access
Open Access at PMChttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC7517343
Indirect radiolabelling has for a long time been the mainstay strategy for radiofluorination of biomolecules. Acylation of biomolecules through the use of an 18F-labelled activated ester is a standard method for indirect radiolabelling. However, the preparation of 18F-labelled activated esters is typically a complex and multistep procedure. Herein, we describe the use of 4-nitrophenyl (PNP) activated esters to rapidly prepare 18F-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.
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