SummaryThree 125 I-labeled 2-O-and 3-O-m-iodobenzyl, and 6-O-m-iodophenyl derivatives of l-ascorbic acid were prepared by melt exchange procedures in isolated radiochemical yields of 12-60% after HPLC purification. Biodistribution studies in tumor-bearing mice showed very different in vivo tissue uptake properties from previous results obtained with 14 C-labeled ascorbic acid and 6-deoxy-6-[ 18 F]fluoro-l-ascorbic acid. None of these seems to be suitable radioiodinated analogs of l-ascorbic acid for imaging study of its in vivo biochemistry.

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Acid. -The title compound (IV) is obtained in a seven-step sequence involving the C5-O-alkylation of alcohol (I) with p-iodobenzyl bromide as the key step. -(KATO, H.; KINO, T.; YAMAMOTO, F.; KANESHIRO, T.; MUKAI, T.; MAEDA*, M.; Chem.