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  • Title: An updated synthesis of N1 '-([11 C]methyl)naltrindole for positron emission tomography imaging of the delta opioid receptor.
    Author: Kaur T, Brooks AF, Hockley BG, Torres J, Henderson BD, Scott PJH, Shao X.
    Journal: J Labelled Comp Radiopharm; 2021 Apr; 64(4):187-193. PubMed ID: 33274468.
    Abstract:
    A new method for the synthesis of the highly selective delta opioid receptor (DOR) antagonist radiotracer N1 '-([11 C]methyl)naltrindole ([11 C]MeNTI) is described. The original synthesis required hydrogenation of a benzyl protecting group after 11 C-labeling, which is challenging in modern radiochemistry laboratories that tend to be heavily automated and operate according to current good manufacturing practice. To address this challenge, we describe development of a novel MeNTI precursor bearing a methoxymethyl acetal (MOM) protecting group, which is easily removed with HCl, and employ it in an updated synthesis of [11 C]MeNTI. The new synthesis is fully automated and validated for clinical use. The total synthesis time is 45 min and provides [11 C]MeNTI in good activity yield (49 ± 8 mCi), molar activity (3,926 ± 326 Ci/mmol) and radiochemical purity (97% ± 2%).
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