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High-yielding, automated radiosynthesis of [ 11 C]martinostat using [ 11 C]methyl triflate.
- Source :
-
Journal of labelled compounds & radiopharmaceuticals [J Labelled Comp Radiopharm] 2022 May 30; Vol. 65 (6), pp. 167-173. Date of Electronic Publication: 2022 Mar 07. - Publication Year :
- 2022
-
Abstract
- Histone deacetylases (HDACs) mediate epigenetic mechanisms implicated in a broad range of central nervous system dysfunction, including neurodegenerative diseases and neuropsychiatric disorders. [ <superscript>11</superscript> C]Martinostat allows in vivo quantification of class I/IIb HDACs and may be useful for the quantification of drug-occupancy relationship, facilitating drug development for disease modifying therapies. The present study reports a radiosynthesis of [ <superscript>11</superscript> C]martinostat using [ <superscript>11</superscript> C]methyl triflate in ethanol, as opposed to the originally described synthesis using [ <superscript>11</superscript> C]methyl iodide and DMSO. [ <superscript>11</superscript> C]Methyl triflate is trapped in a solution of 2 mg of precursor 1 dissolved in anhydrous ethanol (400 μl), reacted at ambient temperature for 5 min and purified by high-performance liquid chromatography; 1.5-1.8 GBq (41-48 mCi; n = 3) of formulated [ <superscript>11</superscript> C]martinostat was obtained from solid-phase extraction using a hydrophilic-lipophilic cartridge in a radiochemical yield of 11.4% ± 1.1% (nondecay corrected to trapped [ <superscript>11</superscript> C]MeI), with a molar activity of 369 ± 53 GBq/μmol (9.97 ± 1.3 Ci/μmol) at the end of synthesis (40 min) and validated for human use. This methodology was used at our production site to produce [ <superscript>11</superscript> C]martinostat in sufficient quantities of activity to scan humans, including losses incurred from decay during pre-release quality control testing.<br /> (© 2022 John Wiley & Sons, Ltd.)
Details
- Language :
- English
- ISSN :
- 1099-1344
- Volume :
- 65
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Journal of labelled compounds & radiopharmaceuticals
- Publication Type :
- Academic Journal
- Accession number :
- 35218059
- Full Text :
- https://doi.org/10.1002/jlcr.3968