Synthesis and Evaluation in Monkey of [18F]4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([18F]FIMX): A Promising Radioligand for PET Imaging of Brain Metabotropic Glutamate Receptor 1 (mGluR1) was written by Xu, Rong;Zanotti-Fregonara, Paolo;Zoghbi, Sami S.;Gladding, Robert L.;Woock, Alicia E.;Innis, Robert B.;Pike, Victor W.. And the article was included in Journal of Medicinal Chemistry in 2013.Recommanded Product: 932738-80-2 The following contents are mentioned in the article:
We sought to develop a PET radioligand that would be useful for imaging human brain metabotropic subtype 1 receptors (mGluR1) in neuropsychiatric disorders and in drug development. 4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)-thiazol-2-yl)-benzamide (FIMX) was identified as having favorable properties for development as a PET radioligand. We developed a method for preparing [18F]FIMX in useful radiochem. yield and in high specific activity from [18F]-fluoride ion and an N-Boc-protected (phenyl)aryliodonium salt precursor. In baseline experiments in the rhesus monkey, [18F]FIMX gave high brain radioactivity uptake, reflecting the expected distribution of mGluR1 with notably high uptake in cerebellum, which became 47% lower by 120 min after radioligand injection. Pharmacol. challenges demonstrated that a very high proportion of the radioactivity in monkey brain was bound specifically and reversibly to mGluR1. [18F]FIMX is concluded to be an effective PET radioligand for imaging mGluR1 in monkey brain and therefore merits further evaluation in human subjects. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2Recommanded Product: 932738-80-2).
4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Recommanded Product: 932738-80-2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica