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A rapid one-step radiosynthesis of [11C]-d-threo-methylphenidate

✍ Scribed by Matthew D. Moran; Alan A. Wilson; Winston T. Stableford; Min Wong; Armando Garcia; Sylvain Houle; Neil Vasdev

Publisher
John Wiley and Sons
Year
2010
Tongue
French
Weight
174 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Carbon‐11 labelled d‐threo‐methylphenidate ([^11^C]‐(1)), a radiopharmaceutical commonly used to image the dopamine transporter, has been labelled in one step using [^11^C]‐methyl triflate. No protection of the nitrogen atom on the piperidine ring of d‐threo‐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.

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