A rapid one-step radiosynthesis of (~(11)C)-d-threo-methylphenidate

摘要

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 centre dot 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.