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The radiosynthesis of a new potential glucose transport protein tracer: 3-[125I]iodophloretin

✍ Scribed by J. Mertens; D. Terriere; R. Boumon

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
492 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Phloretin (2′,4′,6′‐trihydroxy‐3‐(4‐hydroxyphenyl)‐propiophenone) is a glucose transport (GLUT) blocker acting at the extracellular part of the GLUT protein. Labelling this compound with radioiodine can provide a tracer for elucidating in vitro and in vivo the role of GLUT's in cells showing an increased glucose metabolism. As the inhibition of GLUT by phloretin is supposed to occur at the 2′,4′,6′‐trihydroxyphenyl site, the radioiodine is substituted on the 3‐position of the 4‐hydroxyphenyl group. Direct electrophilic substitution on this position is not possible due to highly activated sites in the trihydroxyphenyl group. 3‐Bromophloretin, the precursor for radioiodination, is prepared using a new method, a saturation substitution followed by the elimination of the unstable bromine atoms. Radioiodinated phloretin is obtained with a labelling yield of 75% by applying Cu^+1^‐assisted radioiodo for bromo exchange at 140°C. Pure non carrier added tracer results from HPLC separation coupled to a mini‐column preconcentration and recovery (± 70% overall yield).

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