J. Mertens, R. Boumon, P. Steegmans
May 1, 2001
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0
Influential Citations
1
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
2-Bromo-phloretinic acid (2-Br-PLA): 2-bromo-4-(3-oxo-3(2,4,6-trihydroxyphenyl) propyl)benzoic acid, the precursor molecule for the radiosynthesis of 2-radioiodophloretinic acid (2-*I-PLA): 2-radioiodo-4-(3-oxo-3(2, 4, 6-trihydroxyphenyl)-propyl)benzoic acid, was prepared by a twelve step synthesis starting from hydrocinnamic acid. The radiosynthesis was carried out by applying the Cu(I)-assisted nucleophilic non-isotopic exchange reaction in acidic reducing medium. The amount of copper to reach high yields was found to be critical. At substrate to copper ratios generally used in this type of synthesis dehalogenation of the starting compound occurred, decreasing the labelling yield considerably. In optimal conditions a labelling yield of 95% was reached.