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
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
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
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
Fluorinated Derivatives of AG-881 for Positron Emission Tomography Detection of Mutated Isocitrate Dehydrogenase 1 [PDF]
Background/Objectives: Since 2016, the mutation of isocitrate dehydrogenase 1 (mIDH1) enzymes has become a major molecular marker for glioma classification and diagnosis. Moreover, the recent success of the INDIGO clinical trial on AG-881 (vorasidenib®),
Thu Hang Lai +6 more
doaj +2 more sources
Automation of Copper-Mediated 18F-Fluorination of Aryl Pinacol Boronates Using 4-Dimethylaminopyridinium Triflate [PDF]
Currently, the copper-mediated radiofluorination of aryl pinacol boronates (arylBPin) using the commercially available, air-stable Cu(OTf)2Py4 catalyst is one of the most efficient synthesis approaches, greatly facilitating access to a range of ...
Mikhail A. Nadporojskii +4 more
doaj +2 more sources
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 +2 more sources
Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes [PDF]
Positron emission tomography (PET) is an advanced biomedical imaging modality that relies on well-designed radiotracers to report on specific protein targets and processes occurring in living animals and humans. Cyclotron-produced short-lived fluorine-18
Qunchao Zhao +3 more
doaj +2 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

