Improved synthesis of 6-bromo-7-[ 11 C]methylpurine for clinical use.
Autor: | Okamura T; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan. okamura.toshimitsu@qst.go.jp., Kikuchi T; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan., Ogawa M; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan.; SHI Accelerator Service, Ltd., 7-1-1 Nishigotanda, Shinagawa-ku, Tokyo, 141-0031, Japan., Zhang MR; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan. |
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Jazyk: | angličtina |
Zdroj: | EJNMMI radiopharmacy and chemistry [EJNMMI Radiopharm Chem] 2024 Feb 09; Vol. 9 (1), pp. 10. Date of Electronic Publication: 2024 Feb 09. |
DOI: | 10.1186/s41181-024-00240-8 |
Abstrakt: | Background: Multidrug resistance-associated protein 1 (MRP1), an energy-dependent efflux pump, is expressed widely in various tissues and contributes to many physiological and pathophysiological processes. 6-Bromo-7-[ 11 C]methylpurine ([ 11 C]7m6BP) is expected to be useful for the assessment of MRP1 activity in the human brain and lungs. However, the radiochemical yield (RCY) in the synthesis of [ 11 C]7m6BP was low, limiting its clinical application, because the methylation of the precursor with [ 11 C]CH Results: [ 11 C]7m6BP was manually synthesized via the methylation of 6-bromopurine with [ 11 C]CH Conclusions: The use of THF, 2-MeTHF, and AcOEt improved the [ 11 C]7m6BP/[ 11 C]9m6BP selectivity in the methylation reaction, and the improved method provided [ 11 C]7m6BP with sufficient radioactivity for clinical use. (© 2024. The Author(s).) |
Databáze: | MEDLINE |
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