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Fully automated radiosynthesis of [1‐(2‐[ 18 F]fluoroethyl),1 H [1,2,3]triazole 4‐ethylene] triphenylphosphonium bromide as a potential positron emission tomography tracer for imaging apoptosis
Author(s) -
Haslop Anna,
Gee Antony,
Plisson Christophe,
Long Nicholas
Publication year - 2013
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3024
Subject(s) - chemistry , radiosynthesis , bromide , phosphonium , azide , radiochemistry , cycloaddition , nuclear chemistry , ethylene , yield (engineering) , positron emission tomography , polymer chemistry , organic chemistry , nuclear medicine , catalysis , medicine , materials science , metallurgy
A novel phosphonium salt bearing a fluorine‐18 labelled triazole has been designed as a potential imaging agent for apoptosis. The radiosynthesis of [1‐(2‐[ 18 F]fluoroethyl),1 H [1,2,3]triazole 4‐ethylene] triphenylphosphonium bromide ([ 18 F]MitoPhos_01) has been carried out on a fully automated system in a two‐step reaction. Radiolabelling an ethyl azide and then carrying out a copper‐mediated 1,3‐cycloaddition reaction has allowed for total synthesis time to be slightly more than 1 h from aqueous [ 18 F]fluoride. After purification by HPLC, the average radiochemical yield was determined to be 9% (not decay corrected); the specific activity was on average 70 GBq/µmol at the end of synthesis, and the radiochemical purity was >99%.