Automated synthesis of 1-[11C]acetoacetate on a TRASIS AIO module. (November 2017)

• Record Type: Journal Article
• Authors: Solingapuram Sai, Kiran Kumar; Donald Gage, H.; Almaguel, Frankis; Neth, Bryan; Hughes, Timothy M.; Tremblay, Sebastien; Castellano, Christian-Alexandre; Cunnane, Stephen C.; Jorgensen, Matthew J.; Craft, Suzanne; Mintz, Akiva
• Is Part Of: Applied radiation and isotopes. Volume 129(2017:Nov.)
• Page Start: 57
• Page End: 61
• Publication Date: 2017-11
• Subjects: [11C]AcAc 1-[11C]acetoacetate -- FDG 2-[18F]fluoro-D-glucose -- PET Positron Emission Tomography -- NHP Non-Human Primate -- EOS End Of Synthesis; Automation -- Ketone metabolism -- PET imaging -- Ion-exchange column -- Formulations -- Non-Human primates; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2017.07.066
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: We automated radiochemical synthesis of 1-[ 11 C]acetoacetate in a commercially available radiochemistry module, TRASIS AllInOne by [ 11 C]carboxylation of the corresponding enolate anion generated in situ from isopropenylacetate and MeLi, and purified by ion-exchange column resins.1-[ 11 C]acetoacetate was synthesized with high radiochemical purity (95%) and specific activity (~ 66.6 GBq/µmol, n = 30) with 35% radiochemical yield, decay corrected to end of synthesis. The total synthesis required ~ 16 min. PET imaging studies were conducted with 1-[ 11 C]acetoacetate in vervet monkeys to validate the radiochemical synthesis. Tissue uptake distribution was similar to that reported in humans. Highlights: Automated and simplified production of 1-[ 11 C]acetoacetate using TRASIS AIO module. 1-[ 11 C]acetoacetate radiochemistry can be directly translated and easily adapted to any automated modules for human injections. 1-[ 11 C]acetoacetate production was validated through monkey PET imaging studies for the first time.