An updated synthesis of N 1 ′‐([ 11 C]methyl)naltrindole for positron emission tomography imaging of the delta opioid receptor
| العنوان: | An updated synthesis of N 1 ′‐([ 11 C]methyl)naltrindole for positron emission tomography imaging of the delta opioid receptor |
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| المؤلفون: | Brian G. Hockley, Xia Shao, Jovany Torres, Tanpreet Kaur, Peter Scott, Bradford D. Henderson, Allen F. Brooks |
| المصدر: | Journal of Labelled Compounds and Radiopharmaceuticals. 64:187-193 |
| بيانات النشر: | Wiley, 2020. |
| سنة النشر: | 2020 |
| مصطلحات موضوعية: | 01 natural sciences, Biochemistry, Medicinal chemistry, 030218 nuclear medicine & medical imaging, Analytical Chemistry, δ-opioid receptor, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Naltrindole, Drug Discovery, medicine, Radiology, Nuclear Medicine and imaging, Protecting group, Spectroscopy, medicine.diagnostic_test, 010405 organic chemistry, Organic Chemistry, Acetal, Antagonist, Total synthesis, Highly selective, 0104 chemical sciences, chemistry, Positron emission tomography, medicine.drug |
| الوصف: | 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%). |
| تدمد: | 1099-1344 0362-4803 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::6c276c7f683e16981df170a1b2cb1aff https://doi.org/10.1002/jlcr.3898 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi...........6c276c7f683e16981df170a1b2cb1aff |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 10991344 03624803 |
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