Results 1 to 10 of about 2,439 (149)

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

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

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

Lewis Acid-Facilitated Radiofluorination of MN3PU: A LRRK2 Radiotracer

Molecules, 2020
Background: Temperature-sensitive radiopharmaceutical precursors require lower reaction temperatures (
Ralf Schirrmacher
exaly   +3 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

Closing the gap between 19F and 18F chemistry [PDF]

EJNMMI Radiopharmacy and Chemistry, 2021
Positron emission tomography (PET) has become an invaluable tool for drug discovery and diagnosis. The positron-emitting radionuclide fluorine-18 is frequently used in PET radiopharmaceuticals due to its advantageous characteristics; hence, methods ...
Javier Ajenjo, Gianluca Destro, Bart Cornelissen, Véronique Gouverneur   +3 more
doaj   +2 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

Ethyl Pinacol Boronates as Advantageous Precursors for Copper-Mediated Radiofluorination. [PDF]

Org Lett
(Hetero)­aryl pinacol boronic esters are routinely used for 18F-labeling and have accelerated numerous diagnostic and drug discovery programs. An analysis of the current state-of-play, however, highlights a pending challenge.
Hadjipaschalis N, Ortalli S, Chen Z, Paton RS, Ford J, Tredwell M, Gouverneur V.   +6 more
europepmc   +4 more sources

Synthesis of a [¹⁸F]F Estradiol Derivative via Click Chemistry Using an Automated Synthesis Module: In Vitro Evaluation as Potential Radiopharmaceutical for Breast Cancer Imaging [PDF]

Pharmaceuticals
“Click reactions” are a very useful tool for the selective conjugation of different molecular subunits to produce complex structures in a simple way. In this paper, we present the application of Cu(I)-catalyzed biorthogonal reactions between alkynes and ...
María Emilia Tejería, María Pía Pereira, Juan Pablo Gambini, Pablo Duarte, Javier Gabriel Giglio, Ana María Rey   +5 more
doaj   +2 more sources