Synthesis of carbon-11-labeled aminoalkylindole derivatives as new candidates of cannabinoid receptor radioligands for PET imaging of alcohol abuse |
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| Affiliation: | 1. Toronto Rehabilitation Institute, Toronto, ON, Canada;2. Depart of Mechanical and Aerospace Engineering, Carleton University, Ottawa, ON, Canada;3. Faculty of Kinesiology, University of New Brunswick, Fredericton, NB, Canada;4. School of Human Kinetics and Recreation, Memorial University of Newfoundland, St. John''s, NL, Canada;1. Department of Chemistry, College of Chemical Engineering and Technology, Wuhan University of Science and Technology, Wuhan, Hubei 430081, PR China;2. Department of Chemistry, University of California, One Shields Ave, Davis, CA 95616, United States;3. Department of Medicine, University of California, San Francisco, CA 94143-0521, United States;4. Department Physiology, University of California, San Francisco, CA 94143-0521, United States;1. Department of Medicinal Chemistry, School of Pharmacy, Health Science Center, Xi’an Jiaotong University, Xi’an, Shaanxi 710061, PR China;2. Department of Pharmacology, School of Basic Medical Sciences, Health Science Center, Xi’an Jiaotong University, Xi’an, Shaanxi 710061, PR China;1. Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA;2. Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA;3. Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA;4. Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA;5. Vanderbilt Institute of Chemical Biology, Vanderbilt University/Vanderbilt University Medical Center, Nashville, TN 37232, USA;1. Shenzhen University Cancer Research Center, Institute of Otorhinolaryngology, Shenzhen 518060, China;2. Sun Yat-sen University Cancer Center, Guangzhou 510060, China |
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| Abstract: | Carbon-11-labeled aminoalkylindole derivatives (1-butyl-7-[11C]methoxy-1H-indol-3-yl)(naphthalene-1-yl)methanone ([11C]3), 1-butyl-7-[11C]methoxy-3-(naphthalene-1-ylmethyl)-1H-indole ([11C]5), and 1-butyl-7-[11C]methoxy-3-(naphthalene-2-yl)-1H-indole ([11C]8) were prepared by O-[11C]methylation of their corresponding precursors with [11C]CH3OTf under basic condition (2 N NaOH) and isolated by a simplified solid-phase extraction (SPE) method in 50–60% radiochemical yields based on [11C]CO2 and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 23 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 185–555 GBq/μmol. |
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| Keywords: | Carbon-11-labeled aminoalkylindole derivatives Radiosynthesis Positron emission tomography (PET) Cannabinoid receptor Alcohol abuse |
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