使用 GE FX 合成模块通过“环内”C-羰基化反应自动化合成 C 标记的羧酸和酯。
Automated production of C-labeled carboxylic acids and esters via "in-loop" C-carbonylation using GE FX synthesis modules.
机构信息
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, Ann Arbor, Michigan, USA.
Interdepartmental Program in Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan, USA.
出版信息
J Labelled Comp Radiopharm. 2024 May 30;67(6):217-226. doi: 10.1002/jlcr.4058. Epub 2023 Aug 22.
An in-loop C-carbonylation process for the radiosynthesis of C-carboxylic acids and esters from halide precursors has been developed. The reaction proceeds at room temperature under mild conditions and enables C-carbonylation of both electron deficient and electron rich (hetero)aromatic halides to provide C-carboxylic acids and esters in good to excellent radiochemical yields, high radiochemical purity, and excellent molar activity. The process has been fully automated using commercial radiochemistry synthesis modules, and application to clinical production is demonstrated via validated cGMP radiosyntheses of [C]bexarotene and [C]acetoacetic acid.
已经开发出一种用于从卤代前体制备 C-羧酸和酯的环内 C-羰基化反应。该反应在室温下温和条件下进行，能够使缺电子和富电子（杂）芳族卤化物进行 C-羰基化，以良好至优秀的放射化学产率、高放射化学纯度和优异的摩尔活性提供 C-羧酸和酯。该过程已使用商业放射性化学合成模块实现完全自动化，并通过经过验证的 cGMP [C]bexarotene 和 [C]乙酰乙酸的放射性合成证明了其在临床生产中的应用。
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