Abstract
R-(−)-[ 11C]Epinephrine ([ 11C]EPI) has been synthesized from R-(−)-norepinephrine by direct methylation with [ 11C]methyl iodide or [ 11C]methyl triflate. The total synthesis time including HPLC purification was 35–40 min. The radiochemical yields (EOB) were 5–10% for [ 11C]methyl iodide and 15–25% for [ 11C]methyl triflate. Radiochemical purity was >98%; optical purity determined by radio-chiral HPLC was >97%. The [ 11C]methyl triflate technique produces R-(−)-[ 11C]epinephrine in quantities (80–170 mCi) sufficient for multiple positron emission tomography studies in humans. The two synthetic methods are generally applicable to the production of other N-[ 11C]methyl phenolamines and N-[ 11C]methyl catecholamines.
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