Synthesis of carbon-11-labeled piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as new selective PET sigma1 receptor probes.
Carbon-11-labeled piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives were first designed and synthesized as new selective PET sigma(1) receptor probes. The target tracers were prepared by O-[(11)C]methylation of their corresponding phenolic hydroxyl precursors using [(11)C]CH(3)OTf under basic conditions and isolated by a simplified SPE method in 40-50% radiochemical yields based on [(11)C]CO(2) and decay corrected to EOB. The overall synthesis time from EOB was 15-20 min, the radiochemical purity was >99%, and the specific activity at EOS was 111-185 GBq/micromol.
Gao
Mingzhang
M
Department of Radiology, Indiana University School of Medicine, Indianapolis, IN 46202-2111, USA.
Wang
Min
M
Hutchins
Gary D
GD
Zheng
Qi-Huang
QH
D002250:Carbon Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling / Q000379:methods; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D017480:Receptors, sigma / Q000032:analysis*; D052616:Solid Phase Extraction; D021241:Spectrometry, Mass, Electrospray Ionization
D002250:Carbon Radioisotopes; D009281:Naphthalenes; D010880:Piperidines; D019275:Radiopharmaceuticals; D017480:Receptors, sigma; C082155:2-methoxynaphthalene