TY  - JOUR
AU  - Haskali, MB
AU  - Farnsworth, AL
AU  - Roselt, PD
AU  - Hutton, CA
Y2  - 2020/11/27
Y1  - 2020/08/01
SN  - 2632-8682
UR  - http://hdl.handle.net/11343/252483
AB  - 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.
LA  - English
PB  - ROYAL SOC CHEMISTRY
T1  - 4-Nitrophenyl activated esters are superior synthons for indirect radiofluorination of biomolecules
DO  - 10.1039/d0md00140f
IS  - RSC Medicinal Chemistry
VL  - 11
IS  - 8
SP  - 919-922
L1  - /bitstream/handle/11343/252483/d0md00140f.pdf?sequence=1&isAllowed=y
ER  -