Issue 8, 2020

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

Abstract

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.

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

Supplementary files

Article information

Article type
Research Article
Submitted
30 Apr 2020
Accepted
28 May 2020
First published
07 Jul 2020
This article is Open Access
Creative Commons BY-NC license

RSC Med. Chem., 2020,11, 919-922

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

M. B. Haskali, A. L. Farnsworth, P. D. Roselt and C. A. Hutton, RSC Med. Chem., 2020, 11, 919 DOI: 10.1039/D0MD00140F

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