Synthesis of Diverse 11C-Labeled PET Radiotracers via Direct Incorporation of [11C]CO2

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• 作者：Andrew V. Mossine ; Allen F. Brooks ; Isaac M. Jackson ; Carole A. Quesada ; Phillip Sherman ; Erin L. Cole ; David J. Donnelly ; Peter J. H. Scott ; Xia Shao
• 刊名：Bioconjugate Chemistry
• 出版年：2016
• 出版时间：May 18, 2016
• 年：2016
• 卷：27
• 期：5
• 页码：1382-1389
• 全文大小：396K
• 年卷期：0
• ISSN：1520-4812

文摘

Three new positron emission tomography (PET) radiotracers of interest to our functional neuroimaging and translational oncology programs have been prepared through new developments in [¹¹C]CO₂ fixation chemistry. [¹¹C]QZ (glutaminyl cyclase) was prepared via a tandem trapping of [¹¹C]CO₂/intramolecular cyclization; [¹¹C]tideglusib (glycogen synthase kinase-3) was synthesized through a tandem trapping of [¹¹C]CO₂ followed by an intermolecular cycloaddition between a [¹¹C]isocyanate and an isothiocyanate to form the 1,2,4-thiadiazolidine-3,5-dione core; [¹¹C]ibrutinib (Bruton’s tyrosine kinase) was synthesized through a HATU peptide coupling of an amino precursor with [¹¹C]acrylic acid (generated from [¹¹C]CO₂ fixation with vinylmagnesium bromide). All radiochemical syntheses are fully automated on commercial radiochemical synthesis modules and provide radiotracers in 1–5% radiochemical yield (noncorrected, based upon [¹¹C]CO₂). All three radiotracers have advanced to rodent imaging studies and preliminary PET imaging results are also reported.