Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1 was written by Yamasaki, Tomoteru;Fujinaga, Masayuki;Yoshida, Yuichiro;Kumata, Katsushi;Yui, Joji;Kawamura, Kazunori;Hatori, Akiko;Fukumura, Toshimitsu;Zhang, Ming-Rong. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Category: thiazole The following contents are mentioned in the article:
The purpose of this study was to develop 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([18F]I) as a new PET ligand for imaging metabotropic glutamate receptor subtype 1 (mGluR1). [18F]I was synthesized by [18F]fluorination of a novel nitro precursor with [18F]KF in the presence of Kryptofix 222. At the end of synthesis, 429-936 MBq (n = 8) of [18F]I was obtained with >99% radiochem. purity and 204-559 GBq/μmol specific activity starting from 6.7 to 13.0 GBq of [18F]F–. The brain distribution of [18F]I was determined by the in vitro and ex vivo autoradiog. using rat brain sections. The in vitro and in vivo specific binding of [18F]I to mGluR1 was detected in the cerebellum, thalamus, hippocampus, and striatum. These results suggest that [18F]I is a promising PET ligand for the in vivo evaluation of mGluR1. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2Category: thiazole).
4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica