N,N-Diethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide
CAS Number:
325142-99-2
Molecular Formula:
C17H26BNO3
4-Nitrophenyl activated esters are superior synthons for indirect radiofluorination of biomolecules
Literature Information
Publication Date
2020-07-07
DOI
10.1039/D0MD00140F
Impact Factor
0
Authors
Peter D. Roselt
View Original
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.
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Source Journal
Recommended Compounds
3-Chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinamine
CAS Number:
1032758-99-8
Molecular Formula:
C11H16BClN2O2
![4-Chloro-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine structure](https://static.chemtradehub.com/structs/869/869335-75-1-a9d0.webp "4-Chloro-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine structure")
4-Chloro-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine
CAS Number:
869335-75-1
Molecular Formula:
C8H4ClF3N2
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