Abstract
AbstractA delta opioid receptor antagonist, N1′‐methylnaltrindole (MeNTI), has been labeled with carbon‐11. The precursor for radiolabeling was prepared in 71% yield by benzylation of the phenolic moiety of naltrindole. Alkylation of the indole nitrogen using [11C]iodomethane and aqueous tetra(n‐butyl)ammonium hydroxide at 80 °C in dimethylformamide followed by hydrogenolysis (H2, 10% Pd‐C) of the benzyl protecting group gave [11C]MeNTI. The average (n = 10) time for radiosynthesis, HPLC purification and formulation was 24 min from end‐of‐bombardment. [11C]MeNTI of high radiochemical purity was obtained at end‐of‐synthesis with an average specific activity of 2050 mCi/μmol and radiochemical yield, based on [11C]iodomethane, of 6%.
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