Synthesis of carbon-11-labeled tricyclic necroptosis inhibitors as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha).
Carbon-11-labeled tricyclic necroptosis inhibitors were first designed and synthesized as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha). The target tracers were prepared by O-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf under basic conditions and isolated by a simplified SPE method in 50-60% radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 15-20 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 111-185 GBq/micromol.
Gao
Mingzhang
M
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208 Indianapolis, IN 46202, USA.
Lola
Christian M
CM
Wang
Min
M
Miller
Kathy D
KD
Sledge
George W
GW
Hutchins
Gary D
GD
Zheng
Qi-Huang
QH
D002250:Carbon Radioisotopes; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D009336:Necrosis / Q000175:diagnosis / Q000000981:diagnostic imaging*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D014409:Tumor Necrosis Factor-alpha / Q000032:analysis*
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D014409:Tumor Necrosis Factor-alpha