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A rapid one‐step radiosynthesis of [11C]‐d‐threo‐methylphenidate
Authors:Matthew D Moran  Alan A Wilson  Winston T Stableford  Min Wong  Armando Garcia  Sylvain Houle  Neil Vasdev
Institution:1. PET Centre, Centre for Addiction and Mental Health, 250 College Street, Toronto, Ont., Canada M5T 1R8;2. Department of Psychiatry, University of Toronto, 250 College Street, Toronto, Ont., Canada M5T 1R8
Abstract:Carbon‐11 labelled dthreo‐methylphenidate (11C]‐(1)), a radiopharmaceutical commonly used to image the dopamine transporter, has been labelled in one step using 11C]‐methyl triflate. No protection of the nitrogen atom on the piperidine ring of dthreo‐ritalinic acid·HCl was required, as O‐methylation was favored over N‐methylation by performing the methylation in buffered solutions which effectively protonate and protect the amine functionality. The reaction was effectively carried out at room temperature in solution by captive solvent ‘LOOP’ methods or using conventional glass vials. Copyright © 2010 John Wiley & Sons, Ltd.
Keywords:PET  carbon‐11  methyl triflate  methylphenidate
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