Simeon, Fabrice G.; Lee, Jae-Hoon; Morse, Cheryl L.; Stukes, Ian; Zoghbi, Sami S.; Manly, Lester S.; Liow, Jeih-San; Gladding, Robert L.; Dick, Rachel M.; Yan, Xuefeng; Taliani, Sabrina; Costa, Barbara; Martini, Claudia; Da Settimo, Federico; Castellano, Sabrina; Innis, Robert B.; Pike, Victor W. published an article in 2021. The article was titled 《Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising 18F-Labeled Ligand》, and you may find the article in Journal of Medicinal Chemistry.HPLC of Formula: 768-35-4 The information in the text is summarized as follows:
Translocator protein 18 kDa (TSPO) is a biomarker of neuroinflammation. [11C]ER176 robustly quantifies TSPO in the human brain with positron emission tomog. (PET), irresp. of subject genotype. We aimed to develop an ER176 analog with potential for labeling with longer-lived fluorine-18 (t1/2 = 109.8 min). New fluoro and trifluoromethyl analogs of ER176 were prepared through a concise synthetic strategy. These ligands showed high TSPO affinity and low human genotype sensitivity. Each ligand was initially labeled by a generic 11C-methylation procedure, thereby enabling speedy screening in mice. Each radioligand was rapidly taken up and well retained in the mouse brain at baseline after i.v. injection. Preblocking of TSPO showed that high proportions of brain uptake were specifically bound to TSPO at baseline. Overall, the 3-fluoro analog of [11C]ER176 ([11C]3b) displayed the most promising imaging properties. Therefore, a method was developed to label 3b with [18F]fluoride ion. [18F]3b gave similarly promising PET imaging results and deserves evaluation in higher species. The results came from multiple reactions, including the reaction of (3-Fluorophenyl)boronic acid(cas: 768-35-4HPLC of Formula: 768-35-4)
(3-Fluorophenyl)boronic acid(cas: 768-35-4) can be used to make novel liquid crystalline fluorobiphenylcyclohexenes and difluoroterphenyls by palladium-catalyzed cross-couplings also used in the synthesis of o-phenylphenols as potent leukotriene B4 receptor agonists.HPLC of Formula: 768-35-4
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics