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Synthesis of [<sup>11</sup>C]atipamezole, a potential PET ligand for the <i>α</i><sub>2</sub>‐adrenergic receptor in the brain
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References
2001
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Synthesis TimeMolecular PharmacologyNatural Product SynthesisBiochemistryMedicineα 2Mechanism Of ActionReceptor (Biochemistry)NeuropharmacologyOrganic ChemistryHplc PurificationPharmacotherapyNeurosciencePharmacologyNeurochemistryPotential Pet LigandAlpha-adrenergic PharmacologyDrug Analysis
Abstract The α 2 ‐adrenergic receptor antagonist atipamezole has been labelled with carbon‐11 using [ 11 C]formaldehyde and 2‐ethyl‐2‐oxoacetylindane. Various routes are proposed for the synthesis of the latter: oxidation of 2‐acetyl‐2‐ethylindane, hydrolysis of 2‐diethoxy‐2‐indane and oxidation of 2‐diazoacetyl‐2‐ethylindane. The average radiochemical yield of [ 11 C]atipamezole was 24% based on [ 11 C]formaldehyde, and the synthesis time, including HPLC purification and formulation, was 45 min. Copyright © 2002 John Wiley & Sons, Ltd.
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