Automated synthesis of 1-[11C]acetoacetate on a TRASIS AIO module

Kiran Kumar Solingapuram Sai; H Donald Gage; Frankis Almaguel; Bryan Neth; Timothy M Hughes; Sebastien Tremblay; Christian-Alexandre Castellano; Stephen C Cunnane; Matthew J Jorgensen; Suzanne Craft; Akiva Mintz

doi:10.1016/j.apradiso.2017.07.066

Automated synthesis of 1-[¹¹C]acetoacetate on a TRASIS AIO module

Appl Radiat Isot. 2017 Nov:129:57-61. doi: 10.1016/j.apradiso.2017.07.066. Epub 2017 Aug 2.

Affiliations

¹ Department of Radiology, Wake Forest School of Medicine, Winston Salem, NC, USA. Electronic address: ksolinga@wakehealth.edu.
² Department of Radiology, Wake Forest School of Medicine, Winston Salem, NC, USA.
³ Department of Internal Medicine, Wake Forest School of Medicine, Winston Salem, NC, USA.
⁴ Research Center on Aging, Sherbrooke Molecular Imaging Center, Université de Sherbrooke, Sherbrooke, Quebec, Canada.
⁵ Department of Pathology-Comparative Medicine, Wake Forest School of Medicine, USA.

Abstract

We automated radiochemical synthesis of 1-[¹¹C]acetoacetate in a commercially available radiochemistry module, TRASIS AllInOne by [¹¹C]carboxylation of the corresponding enolate anion generated in situ from isopropenylacetate and MeLi, and purified by ion-exchange column resins.1-[¹¹C]acetoacetate was synthesized with high radiochemical purity (95%) and specific activity (~ 66.6GBq/µmol, n = 30) with 35% radiochemical yield, decay corrected to end of synthesis. The total synthesis required ~ 16min. PET imaging studies were conducted with 1-[¹¹C]acetoacetate in vervet monkeys to validate the radiochemical synthesis. Tissue uptake distribution was similar to that reported in humans.

Keywords: Automation; Formulations; Ion-exchange column; Ketone metabolism; Non-Human primates; PET imaging.

Automated synthesis of 1-[¹¹C]acetoacetate on a TRASIS AIO module

Authors

Affiliations

Abstract

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