Molecular Imaging Branch, NIMH, National Institutes of Health , Bethesda, Maryland 20892, United States.
J Org Chem. 2017 Nov 17;82(22):11925-11932. doi: 10.1021/acs.joc.7b01704. Epub 2017 Oct 13.
Pd(0)-mediated C-carbonylation of aryl(mesityl)iodonium salts followed by suitable quench provides a rapid room-temperature two-pot procedure for labeling arylcarboxylic acids and amide derivatives with the short-lived positron emitter carbon-11 (t = 20.4 min) in generally good to high yields (up to 71%). High product ring selectivity (≥13) was achieved when using mesityl as a spectator group in the diaryliodonium salt precursors. This process has potential for preparing new radiotracers for molecular imaging with positron emission tomography.
Pd(0)介导的芳基(均三甲苯基)碘翁盐的 C-羰基化反应，随后进行适当的淬灭，提供了一种快速的室温两步法，可用于用短寿命正电子发射体碳-11（t = 20.4 分钟）标记芳基羧酸和酰胺衍生物，通常产率高（高达 71%）。当使用均三甲苯作为二芳基碘翁盐前体中的旁观基团时，获得了高的产物环选择性（≥13）。该过程有可能制备用于正电子发射断层扫描的新型放射性示踪剂进行分子成像。
