Aryltrimethylammonium trifluoromethanesulfonates as precursors to aryl [<SUP><FONT size=-1>18</FONT></SUP>F]fluorides: Improved synthesis of [<SUP><FONT size=-1>18</FONT></SUP>F]GBR-13119
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19
摘要:
Aromatic nucleophilic substitution of various trimethylammonium trifluoromethanesulfonates with [ 18 F]fluoride has been evaluated. Fluorinations were studied over a temperature range of 45-165°C, with decay corrected yields ranging from 20-80%. [ 18 F]GBR 13119, 1-[2-{(4-[ 18 F]fluorophenyl)(phenyl)methoxy}ethyl]-4-(3-phenylpropyl)piperazine, a potential radio-tracer for the dopamine uptake system, has been prepared in no-carrier-added form from 4-N,N,N,-trimethylaniliniumphenylmethanone trifluoromethanesulfonate. Purification by solid-phase techniques yielded the product in 20% decay corrected radiochemical yield and >98% radiochemical and chemical purity without HPLC.
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关键词:
Trimethylammonium trifluoromethanesulfonates Fluorine-18 [18F]GBR 13119 Aromatic nucleophilic substitution
DOI:
10.1002/jlcr.2580270711
年份:
1989
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