Results 11 to 20 of about 1,138 (121)

Aryl and Alkyl Radiotrifluoromethylation via Metallaphotoredox‐Mediated Radical Cross‐Coupling [PDF]

Angewandte Chemie, Volume 138, Issue 16, 13 April 2026.
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
Lukas Veth, Albert D. Windhorst, Danielle J. Vugts   +2 more
wiley   +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]

Pharmaceuticals
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, Thomas Wicher, Boris D. Zlatopolskiy, Johannes Ermert, Bernd Neumaier   +4 more
doaj   +2 more sources

25 Years of “Loop” Radiochemistry for PET Imaging [PDF]

Journal of Labelled Compounds and Radiopharmaceuticals, Volume 69, Issue 4-6, April‐May 2026.
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.
Emily Murrell, Sahil Khan, Neil Vasdev
wiley   +2 more sources

18F‐Radiopharmaceutical Diversification Enabled by Deaminative Cross‐Electrophile Couplings [PDF]

Angewandte Chemie, Volume 138, Issue 4, 22 January 2026.
A general Ni‐mediated (C)sp2–(C)sp3 cross‐coupling expedites access to 18F‐radiopharmaceuticals, essential for positron emission tomography imaging and drug discovery. This late‐stage diversification approach was implemented across three user‐friendly automated protocols affording 18F‐radiotracers in sufficient quantities for imaging.
Isabella F. Ogilvy, Joseph Ford, Sebastiano Ortalli, Evelien Renders, Thomas R. Hayes, Shuanglong Liu, Inne Mortiers, Anastasia Nikolopoulou, Alexandre M. Sorlin, Andrés A. Trabanco, Matthew Tredwell, Peter J. J. A. Buijnsters, Rhys Salter, Véronique Gouverneur   +13 more
wiley   +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]

Pharmaceuticals
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, Olga S. Fedorova, Nikolai B. Viktorov, Raisa N. Krasikova   +3 more
doaj   +2 more sources

A simplified, robust protocol for [18F]fluoride elution under mild conditions to enhance late-stage aromatic radiofluorinations [PDF]

Scientific Reports
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, Alexandros Pappas, Niki Constantinou, Staffan Holmin, Jeroen A. C. M. Goos   +4 more
doaj   +2 more sources

Triflyl [18F]Fluoride as a Solution for Base‐Sensitive Late‐Stage Nucleophilic Aromatic 18F‐Fluorination Reactions [PDF]

Chemistry – A European Journal, Volume 31, Issue 2, January 9, 2025.
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 ...
Lizeth Y. F. Haveman, Anna M. T. de Kruijff, Sjoerd P. P. van Eeden, Albert D. Windhorst, Danielle J. Vugts   +4 more
wiley   +2 more sources

Fluorinated Derivatives of AG-881 for Positron Emission Tomography Detection of Mutated Isocitrate Dehydrogenase 1 [PDF]

Pharmaceuticals
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, Sladjana Dukić-Stefanović, Winnie Deuther-Conrad, Aurélie Maisonial-Besset, Rodrigo Teodoro, Magali Toussaint, Barbara Wenzel   +6 more
doaj   +2 more sources

Automation of Copper-Mediated ¹⁸F-Fluorination of Aryl Pinacol Boronates Using 4-Dimethylaminopyridinium Triflate [PDF]

Molecules
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, Viktoriya V. Orlovskaya, Olga S. Fedorova, Dmitry S. Sysoev, Raisa N. Krasikova   +4 more
doaj   +2 more sources

The hydrogenation side-reaction in copper-mediated radiofluorination [PDF]

EJNMMI Radiopharmacy and Chemistry
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, Barbara Wenzel, Ramona Oehme, Claudia Wiesner, Klaus Kopka, Rareş-Petru Moldovan   +5 more
doaj   +2 more sources