0000000000048352
AUTHOR
Andreas Bauman
Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane
Abstract Radiochemical 18 F-fluorination yields of several compounds using the secondary labelling precursors 2-[ 18 F]fluoroethyl tosylate ([ 18 F]FETos) and 1-bromo-2-[ 18 F]fluoroethane ([ 18 F]BFE) could be considerably enhanced by the addition of an alkali iodide. The radiochemical yield of [ 18 F]fluoroethyl choline for example could be doubled with [ 18 F]BFE and increased from 13% to ≈80% with [ 18 F]FETos. By addition of alkali iodide to the precursor, the 18 F-fluoroethylation yields of established radiopharmaceuticals, especially in the case of automated syntheses, could be significantly increased without major changes of the reaction conditions.
Improved automated synthesis of [18F]fluoroethylcholine as a radiotracer for cancer imaging.
[(18)F]Fluoroethylcholine has been recently introduced as a promising (18)F-labelled analogue of [(11)C]choline which had been previously described as a tracer for metabolic cancer imaging with positron emission tomography (PET). Due to the practical advantages of using the longer-lived radioisotope (18)F (t(1/2)=110 min), offering the opportunity of a more widespread clinical application, we established a reliable, fully automated synthesis for its production using a modified, commercially available module. [(18)F]Fluoroethylcholine was prepared from N,N-dimethylaminoethanol by iodide catalyzed alkylation with 1-[(18)F]fluoro-2-tosylethane as alkylating agent, resulting in a total radioche…
Synthesis, labelling and evaluation of hydantoin-substituted indole carboxylic acids as potential ligands for positron emission tomography imaging of the glycine binding site of the N-methyl-d-aspartate receptor
The N-methyl- d-aspartate (NMDA) receptor as a type of ionotropic glutamatergic receptors is essential for physiological processes such as learning, memory and synaptic plasticity. A glutamate-induced overactivation of these receptors, accompanied by increased intracellular calcium concentration, causes cell injury and leads to a large number of acute or chronic neurological disorders, such as stroke, trauma, Parkinson's disease and Alzheimer's disease. In an attempt to visualise the glutamatergic neurotransmission in vivo with positron emission tomography, novel fluoroethoxy- and methoxy-substituted reference compounds based on the lead structure of a hydantoin-substituted indole-2-carboxy…
On the consensus nomenclature rules for radiopharmaceutical chemistry – Reconsideration of radiochemical conversion
Radiochemical conversion is an important term to be included in the "Consensus nomenclature rules for radiopharmaceutical chemistry". Radiochemical conversion should be used to define reaction efficiency by measuring the transformation of components in a crude reaction mixture at a given time, whereas radiochemical yield is better suited to define the efficiency of an entire reaction process including, for example, separation, isolation, filtration, and formulation. (C) 2020 Elsevier Inc. All rights reserved.