103935-48-4Relevant articles and documents
Synthesis and evaluation of new 18F-labelled acetamidobenzoxazolone-based radioligands for imaging of the translocator protein (18 kDa, TSPO) in the brain
Tiwari, Anjani K.,Fujinaga, Masayuki,Yui, Joji,Yamasaki, Tomoteru,Xie, Lin,Kumata, Katsushi,Mishra, Anil K.,Shimoda, Yoko,Hatori, Akiko,Ji, Bin,Ogawa, Masanao,Kawamura, Kazunori,Wang, Feng,Zhang, Ming-Rong
, p. 9621 - 9630 (2014)
The visualization of the activated microglia/TSPO is one of the main aspects of neuroimaging. Here we describe two new 18F-labelled molecules, 2-[5-(4-[18F]fluoroethoxyphenyl)- ([18F]2) and 2-[5-(4-[18F]fluoropr
Synthetic method for cyclopropyl diphenyl sulfonium trifluoromethanesulfonic salt
-
Paragraph 0029; 0030; 0031; 0032, (2017/08/28)
The invention provides a synthetic method for cyclopropyl diphenyl sulfonium trifluoromethanesulfonic salt. The synthetic method includes the steps that (a) 3-halogen-1-propyl alcohol and trifluoromethanesulfonic anhydride serve as raw materials for synth
Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain
Fujinaga, Masayuki,Yamasaki, Tomoteru,Yui, Joji,Hatori, Akiko,Xie, Lin,Kawamura, Kazunori,Asagawa, Chiharu,Kumata, Katsushi,Yoshida, Yuichiro,Ogawa, Masanao,Nengaki, Nobuki,Fukumura, Toshimitsu,Zhang, Ming-Rong
scheme or table, p. 2342 - 2352 (2012/05/31)
We designed three novel positron emission tomography ligands, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[ 11C]methoxy-N-methylbenzamide ([11C]6), 4-[ 18F]fluoroethoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methylbenzamide ([18F]7), and 4-[ 18F]fluoropropoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methylbenzamide ([18F]8), for imaging metabotropic glutamate receptor type 1 (mGluR1) in rodent brain. Unlabeled compound 6 was synthesized by benzoylation of 4-pyrimidinyl-2-methylaminothiazole 10, followed by reaction with isopropylamine. Removal of the methyl group in 6 gave phenol precursor 12 for radiosynthesis. Two fluoroalkoxy analogues 7 and 8 were prepared by reacting 12 with tosylates 13 and 14. Radioligands [ 11C]6, [18F]7, and [18F]8 were synthesized by O-[11C]methylation or [18F]fluoroalkylation of 12. Compound 6 showed high in vitro binding affinity for mGluR1, whereas 7 and 8 had weak affinity. Autoradiography using rat brain sections showed that [ 11C]6 binding is aligned with the reported distribution of mGluR1 with high specific binding in the cerebellum and thalamus. PET study with [ 11C]6 in rats showed high brain uptake and a similar distribution pattern to that in autoradiography, indicating the usefulness of [ 11C]6 for imaging brain mGluR1.