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Synthesis of a Radiotracer for Studying k‐Subtype Opiate Receptors: N‐[ 11 C‐methyl]‐N‐( trans ‐2‐pyrrolidinyl‐cyclohexyl)‐3,4‐dichlorophenylacetamide ([ 11 C](±)U‐50488H)
Author(s) -
Noble Glen D.,
Dannals Robert F.,
Ravert Hayden T.,
Wilson Alan A.,
Wagner Henry N.
Publication year - 1992
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580310202
Subject(s) - chemistry , chemical synthesis , stereochemistry , medicinal chemistry , radiochemistry , in vitro , biochemistry
Abstract The radiochemical synthesis of a κ‐subtype opiate receptor ligand, [ 11 C](±)U‐50488H, was accomplished either in two steps or by direct methylation with [ 11 C]iodomethane. The radiotracer was purified using reversed phase semipreparative HPLC. The average specific activity was 1830 mCi/μmole (calculated at the end‐of‐synthesis; EOS) for the direct methylation and 2140 mCi/μmole EOS for the two‐step one‐pot synthesis. The average time of synthesis including formulation was approximately 22 minutes for the direct methylation and 27 minutes for the two‐step one‐pot synthesis.