The hydrogenation side-reaction in copper-mediated radiofluorination [PDF]
Background Copper-mediated radiofluorination (CMRF) is a breakthrough in 18F-radiochemistry, enabling 18F incorporation into molecules even at electron-rich aromatic positions. In recent years, several improved protocols have been reported to advance the
Sarandeep Kaur +5 more
doaj +5 more sources
Aryl and Alkyl Radiotrifluoromethylation via Metallaphotoredox-Mediated Radical Cross-Coupling. [PDF]
The metallaphotoredox‐mediated radiotrifluoromethylation of arenes and alkanes is described. The operationally simple protocols make use of substrates bearing thianthrenium salts (TT) or N‐hydroxyphthalimide (NHPI) esters and CF218FI. The reaction proceeds through a Ru‐mediated radical formation followed by a Cu‐mediated radical cross‐coupling step and
Veth L, Windhorst AD, Vugts DJ.
europepmc +3 more sources
Electrochemical Flash Fluorination and Radiofluorination [PDF]
AbstractA new method for rapid late‐stage fluorination using the cation pool technique is presented. Fluorination and no‐carrier‐added radiofluorination of methyl (phenylthio) acetate, methyl 2‐(methylthio) acetate, and methyl 2‐(ethylthio) acetate were performed.
Sam Sadeghi +2 more
exaly +3 more sources
Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes
The polymer supported phosphazene bases PS-P2tBu and the novel PS-P2PEG allowed for efficient extraction of [18F]F− from proton irradiated [18O]H2O and subsequent radiofluorination of a broad range of substrates directly on the resin.
Fedor Zhuravlev
exaly +3 more sources
Fully Automated Production of (((S)-1-Carboxy-5-(6-([18F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic Acid ([18F]JK-PSMA-7) [PDF]
Background: The radiotracer [18F]JK-PSMA-7, a prostate cancer imaging agent for positron emission tomography (PET), was previously synthesized by indirect radiofluorination using an 18F-labeled active ester as a prosthetic group, which had to be isolated
Philipp Krapf +4 more
doaj +2 more sources
Lewis Acid-Facilitated Radiofluorination of MN3PU: A LRRK2 Radiotracer
Background: Temperature-sensitive radiopharmaceutical precursors require lower reaction temperatures (
Paul Schaffer +2 more
exaly +3 more sources
25 Years of "Loop" Radiochemistry for PET Imaging. [PDF]
While conventional methods to 11C‐ and 18F‐labelled radiopharmaceuticals utilize a vial‐based approach, in the past quarter‐century, a modern, efficient, and cleaner “loop method” has been developed. The radiochemical diversity of reactions synthesized by the loop method are shown.
Murrell E, Khan S, Vasdev N.
europepmc +2 more sources
Simple and Efficient Synthesis of N-Succinimidyl-4-[18F]fluorobenzoate ([18F]SFB)—An Important Intermediate for the Introduction of Fluorine-18 into Complex Bioactive Compounds [PDF]
Background: N-succinimidyl-[18F]fluorobenzoate ([18F]SFB) is commonly prepared through a three-step procedure starting from [18F]fluoride ion. A number of methods for the single-step radiosynthesis of [18F]SFB have been introduced recently, including the
Viktoriya V. Orlovskaya +3 more
doaj +2 more sources
A simplified, robust protocol for [18F]fluoride elution under mild conditions to enhance late-stage aromatic radiofluorinations [PDF]
Direct radiofluorination of base-sensitive PET precursors is challenging due to the harsh reaction conditions of traditional fluorine-18 radiochemistry. In particular, the presence of inorganic bases with a relatively high conjugate pK a (e.g. K2CO3) and
Stefan Milton +4 more
doaj +2 more sources
Triflyl [18F]Fluoride as a Solution for Base-Sensitive Late-Stage Nucleophilic Aromatic 18F-Fluorination Reactions. [PDF]
Here, we present the late‐stage nucleophilic 18F‐fluorination of (hetero)aryls under low‐base conditions using triflyl [18F]fluoride. This method avoids the application of base and cryptand and enabled the efficient radiolabeling of a broad scope of (hetero)arenes and the successful production of clinical doses of [18F]mFBG, [18F]SynVesT‐1 and [18F ...
Haveman LYF +4 more
europepmc +2 more sources

