High yield synthesis of high specific activity R-(-)-[11C]epinephrine for routine PET studies in humans.

Autor: Chakraborty PK; Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109-0552., Gildersleeve DL, Jewett DM, Toorongian SA, Kilbourn MR, Schwaiger M, Wieland DM
Jazyk: angličtina
Zdroj: Nuclear medicine and biology [Nucl Med Biol] 1993 Nov; Vol. 20 (8), pp. 939-44.
DOI: 10.1016/0969-8051(93)90094-b
Abstrakt: 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.
Databáze: MEDLINE