In:
Journal of Labelled Compounds and Radiopharmaceuticals, Wiley, Vol. 46, No. 6 ( 2003-05), p. 587-598
Abstract:
[ 18 F]Fluoroethyl bromide ([ 18 F]FEtBr) is a useful synthetic precursor to synthesize 18 F‐labeled compounds. However, the lower reactivity of [ 18 F]FEtBr with amine, phenol and amide functional groups than that of [ 11 C]CH 3 I partly limits its wide application in the synthesis of [ 18 F]fluoroethylated compounds. The aim of this study was to increase the reactivity of [ 18 F]FEtBr with various nucleophilic substrates for PET tracers containing amine, phenol and amide moieties. The present strategies included (1) adding NaI into the reaction mixture of [ 18 F]FEtBr and substrate, where [ 18 F]FEtI is reversibly formed and becomes more reactive; (2) converting [ 18 F]FEtBr into much more reactive [ 18 F]FEtOTf, similar to conversion of [ 11 C]CH 3 I into [ 11 C]CH 3 OTf. By these efforts, the [ 18 F]fluoroethylation efficiency of various substrates containing amine, phenol and amide groups with [ 18 F]FEtBr/NaI and [ 18 F]FEtOTf was significantly improved, compared with the corresponding reaction efficiency with [ 18 F]FEtBr. Copyright © 2003 John Wiley & Sons, Ltd.
Type of Medium:
Online Resource
ISSN:
0362-4803
,
1099-1344
Language:
English
Publisher:
Wiley
Publication Date:
2003
detail.hit.zdb_id:
1491841-9
detail.hit.zdb_id:
196095-7
SSG:
15,3
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