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- W2086454014 abstract "Pd0-Mediated C-[18F]fluoromethylation of pinacolborane-substituted benzoate 1 and [18F]FCH2X (X = Br or I) has been carried out with a focus on the rapid incorporation of a [18F]fluoromethyl group into an aryl carbon framework. The reaction of 1 and [18F]FCH2I under the conditions of [Pd2(dba)3]/P(o-CH3C6H5)3 (1:6) and K2CO3 in DMF at 65 °C for 5 min afforded the [18F]fluoromethylated benzoate [18F]-2 in 23% HPLC analytical yield. The coupling efficiency was significantly enhanced by the reaction of 1 and [18F]FCH2Br under the conditions of [Pd2(dba)3]/P(o-tolyl)3 (1:6) and K2CO3 in DMPU:H2O (9:1) at 120 °C within 15 min to afford [18F]-2 in 64% HPLC analytical yield (up to 86% HPLC analytical yield when strictly controlling the reaction temperature with ±3 °C accuracy) and 66% decay-corrected isolated yield based on [18F]FCH2Br. The total synthesis time starting from the production of 18F− in the cyclotron was 88 min. The reaction was extended to various aryl compounds." @default.
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- W2086454014 date "2012-11-15" @default.
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- W2086454014 title "Pd<sup>0</sup>-Mediated Rapid <i>C</i>-[<sup>18</sup>F]Fluoromethylation by the Cross-Coupling Reaction of a [<sup>18</sup>F]Fluoromethyl Halide with an Arylboronic Acid Ester: Novel Method for the Synthesis of a <sup>18</sup>F-Labeled Molecular Probe for Positron Emission Tomography" @default.
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- W2086454014 doi "https://doi.org/10.1246/bcsj.20120151" @default.
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