Ascorbate Analogs for Use in Medical Imaging:Synthesis and Radical Scavenging Activity of 5-O-(4'-Iodobenzyl)-L-ascorbic Acid

摘要

As part of our program to develop potential imaging agents for ascorbate bioactivity in the brain,5-0-(4'-iodobenzyl)-L-ascorbic acid was prepared through a seven-step sequence which involved C5-O-alkylation with p-iodobenzyl bromide in the presence of Ag2O and CaSO4 as the key step,starting from L-ascorbic acid.The scavenging activity of the p-iodobenzylated analog against 2,2-diphenyl-1-picrylhyrazyl (DPPH) radical was almost the same as that of L-ascorbic acid itself.