Synthesis and biodistribution of F-18 labeled scyllo-inositol derivatives as potential probes for detecting amyloid beta oligomers

TL;DRAbstract

1935 Objectives Scyllo-inositol appears to bind small Aβ oligomers inhibiting their aggregation and deposition as amyloid plaque in the brain. Mechanistic data indicate scyllo-inositol binds and neutralizes these oligomers into soluble complexes while reducing the amount of larger oligomeric species. An F-18 labeled scyllo-inositol derivative may be beneficial as a probe for studying the early formation of amyloid plaque. Here we present two such labeled derivatives and their biodistributions. Methods 1-Deoxy-1-[18F]fluoro-2,3,4,5,6-penta-O-acetyl-scyllo-inositol (1) and 1-deoxy-1-[18F]fluoro-scyllo-inositol (2) were prepared from the benzyl myo-mesylate using K18F/Kryptofix in acetonitrile at 150oC. The crude product was treated with HBr/acetic acid at 250C and after purification furnished the labeled acetylated scyllo-inositol derivative 1. Mild base hydrolysis followed by C18 SepPak purification gave the unprotected labeled compound 2. Biodistributions were performed in normal mice.

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