在TRASIS AIO模块上自动合成1-[C]乙酰乙酸酯。
Automated synthesis of 1-[C]acetoacetate on a TRASIS AIO module.
作者信息
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
机构信息
Department of Radiology, Wake Forest School of Medicine, Winston Salem, NC, USA.
Department of Radiology, Wake Forest School of Medicine, Winston Salem, NC, USA.
出版信息
Appl Radiat Isot. 2017 Nov;129:57-61. doi: 10.1016/j.apradiso.2017.07.066. Epub 2017 Aug 2.
Abstract
We automated radiochemical synthesis of 1-[C]acetoacetate in a commercially available radiochemistry module, TRASIS AllInOne by [C]carboxylation of the corresponding enolate anion generated in situ from isopropenylacetate and MeLi, and purified by ion-exchange column resins.1-[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-[C]acetoacetate in vervet monkeys to validate the radiochemical synthesis. Tissue uptake distribution was similar to that reported in humans.
摘要
我们在市售的放射化学模块TRASIS AllInOne中通过对由乙酸异丙烯酯和甲基锂原位生成的相应烯醇负离子进行[C]羧化反应，实现了1-[C]乙酰乙酸的自动化放射化学合成，并通过离子交换柱树脂进行纯化。1-[C]乙酰乙酸的合成具有高放射化学纯度（95%）和比活度（约66.6GBq/µmol，n = 30），放射化学产率为35%，衰变校正至合成结束。总合成时间约为16分钟。用1-[C]乙酰乙酸在黑长尾猴身上进行了PET成像研究，以验证放射化学合成。组织摄取分布与人类报告的相似。
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