Results 11 to 20 of about 1,195 (160)

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

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

Angew Chem Int Ed Engl
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.
Ogilvy IF, Ford J, Ortalli S, Renders E, Hayes TR, Liu S, Mortiers I, Nikolopoulou A, Sorlin AM, Trabanco AA, Tredwell M, Buijnsters PJJA, Salter R, Gouverneur V.   +13 more
europepmc   +2 more sources

Investigation on the isotopic exchange radiofluorination of the pentafluorosulfanyl group.

Org Biomol Chem
This study reports the first radiofluorination of pentafluorosulfanyl groups  via  isotopic exchange, analyzes reaction conditions with AI and statistical tools, and proposes the formation of positional isotopologues.
Hiscocks H, Weerasinghe G, Huang W, Colasuonno F, Hill J, Ryan P, Johnston R, Brooks A, Scott PJH, Ung A, Lessio M, Hunter L, Pascali G.   +12 more
europepmc   +6 more sources

Late-Stage Copper-Catalyzed Radiofluorination of an Arylboronic Ester Derivative of Atorvastatin

Molecules, 2019
There is an unmet need for late-stage 18F-fluorination strategies to label molecules with a wide range of relevant functionalities to medicinal chemistry, in particular (hetero)arenes, aiming to obtain unique in vivo information on the pharmacokinetics ...
Tryfon Zarganes - Tzitzikas, Gonçalo S Clemente, Philip Elsinga   +2 more
exaly   +3 more sources

Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes [PDF]

Nature Communications
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, Sanjay Telu, Shuiyu Lu, Victor W. Pike   +3 more
doaj   +2 more sources

Generic semi-automated radiofluorination strategy for single domain antibodies: [18F]FB-labelled single domain antibodies for PET imaging of fibroblast activation protein-α or folate receptor-α overexpression in cancer [PDF]

EJNMMI Radiopharmacy and Chemistry
Background Radiofluorination of single domain antibodies (sdAbs) via N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) has shown to be a promising strategy in the development of sdAb-based PET tracers. While automation of the prosthetic group (PG) [18F]SFB
Herlinde Dierick, Laurent Navarro, Hannelore Ceuppens, Thomas Ertveldt, Ana Rita Pombo Antunes, Marleen Keyaerts, Nick Devoogdt, Karine Breckpot, Matthias D’Huyvetter, Tony Lahoutte, Vicky Caveliers, Jessica Bridoux   +11 more
doaj   +2 more sources

Radiosynthesis of 5-[¹⁸F]Fluoro-1,2,3-triazoles through Aqueous Iodine–[¹⁸F]Fluorine Exchange Reaction

Molecules, 2021
In this report, a simple and efficient process to achieve fluorine-18-labeled 1,2,3-triazole is reported. The heteroaromatic radiofluorination was successfully achieved through an iodine–fluorine-18 exchange in an aqueous medium requiring only trace ...
Xiang Zhang, Falguni Basuli, Sameh Abdelwahed, Tadhg Begley, Rolf Swenson   +4 more
doaj   +1 more source

[18F]Tosyl fluoride as a versatile [18F]fluoride source for the preparation of 18F-labeled radiopharmaceuticals

Scientific Reports, 2023
Positron emission tomography (PET) is an in vivo imaging technology that utilizes positron-emitting radioisotope-labeled compounds as PET radiotracers that are commonly used in clinic and in various research areas, including oncology, cardiology, and ...
Dong Zhou, Wenhua Chu, Jinbin Xu, Sally Schwarz, John A. Katzenellenbogen   +4 more
doaj   +1 more source

Mild, Organo-Catalysed Borono-Deamination as a Key to Late-Stage Pharmaceutical Precursors and 18F-Labelled Radiotracers

Frontiers in Chemistry, 2022
A tris(pentafluorophenyl)borane catalysed method for the synthesis of boronic acid esters from aromatic amines in yields of up to 93% was devised.
Raúl M. Pérez-García, Patrick J. Riss, Patrick J. Riss, Patrick J. Riss, Patrick J. Riss   +4 more
doaj   +1 more source