2023
Fully automated radiosynthesis of [18F]mG4P027 for mGluR4 imaging
Moon S, Fakhri G, Zhang Z, Brownell A, Wang J. Fully automated radiosynthesis of [18F]mG4P027 for mGluR4 imaging. IRADIOLOGY 2023, 1: 120-127. PMID: 37496513, PMCID: PMC10371389, DOI: 10.1002/ird3.25.Peer-Reviewed Original Research
2020
Synthesis and Characterization of Fluorine-18-Labeled N‑(4-Chloro-3-((fluoromethyl‑d 2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain
Wang J, Qu X, Shoup T, Yuan G, Afshar S, Pan C, Zhu A, Choi J, Kang H, Poutiainen P, Fakhri G, Zhang Z, Brownell A. Synthesis and Characterization of Fluorine-18-Labeled N‑(4-Chloro-3-((fluoromethyl‑d 2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain. Journal Of Medicinal Chemistry 2020, 63: 3381-3389. PMID: 32081008, PMCID: PMC7261135, DOI: 10.1021/acs.jmedchem.0c00201.Peer-Reviewed Original ResearchConceptsDrug-like propertiesMethylthio analoguePotential ligandsMetabolic stabilityPositron emission tomographyRadiochemical yieldMolar activityDose-dependent blocking effectPositron emission tomography imaging studiesMethylthioPAM activityBrain regionsMale Sprague Dawley ratsLigandEx vivo biodistribution studiesRadiosynthesisSprague Dawley ratsBrainMGluR4SynthesisAnaloguesEmission tomographyImaging studies
2017
A report of the automated radiosynthesis of the tau positron emission tomography radiopharmaceutical, [18F]‐THK‐5351
Neelamegam R, Yokell D, Rice P, Furumoto S, Kudo Y, Okamura N, Fakhri G. A report of the automated radiosynthesis of the tau positron emission tomography radiopharmaceutical, [18F]‐THK‐5351. Journal Of Labelled Compounds And Radiopharmaceuticals 2017, 60: 140-146. PMID: 27859483, DOI: 10.1002/jlcr.3482.Peer-Reviewed Original ResearchConceptsO-THPNucleophilic fluorination reactionsHydrochloric acidFluorination reactionDilute hydrochloric acidSemi-preparative high-performance liquid chromatographyTosylate precursorHigh-performance liquid chromatographyUncorrected radiochemical yieldDimethyl sulfoxideRadiochemical yieldRadiosynthesis moduleMulti-center trialLiquid chromatographyAutomated RadiosynthesisRadiosynthesisPositron emission tomography radiopharmaceuticalsPET imaging agentUnited States Pharmacopeia
2004
Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-β-Carbomethoxy-3-β-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET
Chaly T, Baldwin R, Neumeyer J, Hellman M, Dhawan V, Garg P, Tamagnan G, Staley J, Al-Tikriti M, Hou Y, Zoghbi S, Gu X, Zong R, Eidelberg D. Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-β-Carbomethoxy-3-β-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET. Nuclear Medicine And Biology 2004, 31: 125-131. PMID: 14741577, DOI: 10.1016/s0969-8051(03)00110-0.Peer-Reviewed Original ResearchConceptsBrain uptakeDopamine transporterRegional brain uptakeGood brain uptakeNon-target ratioDAT imagingPlasma metabolite analysisTarget ratioΒ-carbomethoxyHigh uptakeImaging agentVivo propertiesHuman primatesRadiochemical purityHigh targetUptakeParent compoundStriatumMetabolite analysisRadiosynthesis
1998
Stereoconservative synthesis of the enantiomerically pure precursors of [11C](+)‐McN 5652 and [11C](−)‐McN 5652
Huang Y, Mahmood K, Simpson N, Mason N, Mathis C. Stereoconservative synthesis of the enantiomerically pure precursors of [11C](+)‐McN 5652 and [11C](−)‐McN 5652. Journal Of Labelled Compounds And Radiopharmaceuticals 1998, 41: 9-17. DOI: 10.1002/(sici)1099-1344(199801)41:1<9::aid-jlcr47>3.0.co;2-8.Peer-Reviewed Original ResearchBenzoyl thioesterTartrate saltFinal productOne-pot deprotectionSynthetic routeConvenient precursorsReaction sequenceSynthesis yieldDetectable isomerizationPurification procedureThioestersThioethersKey stepSubsequent formationSpecific activityCi/High specific activitySaltHPLC analysisPrecursorsRadiochemical purityS-methylationDeprotectionIsomerizationRadiosynthesis
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