The first synthesis of [11C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3)
作者： Min Wang , Mingzhang Gao , Kathy D. Miller , George W. Sledge , Gary D. Hutchins
DOI: 10.1016/J.BMCL.2010.11.026
关键词:
摘要: SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), new potential PET agent for imaging GSK-3, was first designed synthesized in 20-30% decay corrected radiochemical yield 370-555 GBq/μmol specific activity at end bombardment (EOB). The synthetic strategy to prepare carbon-11-labeled maleic anhydride intermediate followed by the conversion maleimide.
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