Synthesis, Radioiodination and Biological distribution of 5-(5-(tributylstannyl) benzofuran-2-yl) pyridin-2-amine as an amyloid imaging agent

Published on: 26th December, 2017

OCLC Number/Unique Identifier: 7317576309

In this work an efficient method developed for the synthesis of 125I-benzofuran-2-yl) pyridin-2-amine (125IBPA), followed by radioiodination with 125I by using Chloramine-T at pH 8. The reaction proceeds within 10 min at room temperature (20-25°C). The radiochemical yield determined by Thin-Layer Chromatography (TLC) using hexane:ethyl acetate (1:6 v/v) and the purity analyzed by high-performance liquid chromatography using a reversed-phase RP18column and acetonitrile:0.1 M ammonium bicarbonate (pH 7.5) (1:1) as the mobile phase at a flow rate of 1 ml×min−1. The radiochemical yield using aH2O2 oxidant found equal to 96.5% with a radiochemical purity of 125I-BPA of over 96.5%. The biodistribution data in normal mice indicated a high initial uptake of 6.54±0.10 (% ID/g±SD) in the brain within 30 min post-injection. These results promote a further the use of 125I-BPA as a novel agent for brain imaging.
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