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

在TRASIS AIO模块上自动合成1-[(11)C]乙酰乙酸酯

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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 (~ 66.6GBq/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-[(11)C]acetoacetate in vervet monkeys to validate the radiochemical synthesis. Tissue uptake distribution was similar to that reported in humans.

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