The first synthesis of [C-11]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3)

SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM. [C-11]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[C-11]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-555 GBq/mu mol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled maleic anhydride intermediate followed by the conversion to maleimide. (C) 2010 Elsevier Ltd. All rights reserved.