On-line [11C]methylation using [11C]methyl iodide for the automated preparation of 11C-radiopharmaceuticals |
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| Affiliation: | 1. Department of Oncology, University of Alberta, 11560 University Avenue, Edmonton, AB T6G 1Z2, Canada;2. Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, AB T6G 2H1, Canada;1. PET Center, Department of Diagnostic Radiology, Yale University School of Medicine, New Haven, CT, USA;2. Department of Psychiatry, Yale University School of Medicine, New Haven, CT, USA |
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| Abstract: | A novel method for the efficient preparation of 11C-radiopharmaceuticals by on-line [11C]methylation using [11C]methyl iodide has been developed and applied to a rapid, convenient automated system. [11C]Methyl iodide is first trapped in a short column, containing an adsorber and coated substrate, which is connected to an HPLC injector. DMF is then introduced. Alternatively the substrate is added with the DMF. A whole reaction mixture can be easily injected onto an HPLC column for purification by switching the injector valve immediately after the reaction. Thus, radiochemical yields in the preparation of 11C-labeled doxepin, benztropine, cyproheptadine and N-methylspiperone have been improved remarkably and the synthetic procedure simplified. |
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