Radiosynthesis of [¹¹C]LY2795050 for Preclinical and Clinical PET Imaging Using Cu(II)-Mediated Cyanation.

ABSTRACT: Copper-mediated ¹¹C-cyanation reactions have enabled the synthesis of PET radiotracers from a range of readily available precursors and avoid the need to use more toxic Pd catalysts. In this work we adapt our recently developed ¹¹C-cyanation of arylpinacolboronate (BPin) esters for the cGMP synthesis of [¹¹C]LY2795050, a selective antagonist radiotracer for the kappa opioid receptor (KOR). [¹¹C]LY2795050 was synthesized in 6 ± 1% noncorrected radiochemical yield (based on [¹¹C]HCN, n = 3) using an automated synthesis module. Quality control testing confirmed the suitability of doses for preclinical and clinical PET imaging (radiochemical purity >99%; specific activity >900 mCi/μmol; residual Cu < 0.1 μg/mL). PET imaging was cond

SUBMITTER: Yang L 

PROVIDER: S-EPMC6295869 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature