Abstract
Peripheral benzodiazepine receptor (PBR) is associated with neuroinflammation and tumor progression. [ 11C]DAA1106 and [ 18F]FEDAA1106 are two promising radioligands for positron emission tomography (PET) imaging of PBR. This study was designed to develop a new radiolabeled analog of [ 11C]DAA1106 and [ 18F]FEDAA1106, [ 11C]FEDAA1106, for PET imaging of PBR expression in brain and cancer. Precursor N-(5-fluoro-2-phenoxyphenyl)- N-(2-(2-fluoroethoxy)-5-hydroxybenzyl)acetamide ( 9) was synthesized in multiple steps with moderate to high chemical yields. Precursor 9 was labeled by [ 11C]CH 3OTf and isolated by high pressure liquid chromatography (HPLC) purification to provide target radioligand N-(5-fluoro-2-phenoxyphenyl)- N-(2-(2-fluoroethoxy)-5-[ 11C]methoxybenzyl)acetamide ([ 11C]FEDAA1106, [ 11C] 10) in 60–70% radiochemical yields, decay corrected to end of bombardment (EOB), based on [ 11C]CO 2. The specific activity of the target radiotracer [ 11C] 10 was in a range of 111–185 GBq/μmol at the end of synthesis (EOS).
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