937183-61-4Relevant articles and documents
Synthesis method for one-pot preparation of N-Boc-N-methyl-4-aminostyrene
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Paragraph 0029-0031, (2020/08/22)
The invention relates to a synthesis method for one-pot preparation of N-Boc-N-methyl-4-aminostyrene. The invention mainly aims to solve the problems of expensive raw materials and high cost in existing methods for synthesizing N-Boc-N-methyl-4-aminostyrene. The synthesis method comprises the following steps: adding a substrate, a methylation reagent, alkali and a dry organic solvent into a reactor for a reaction, and after the reaction is finished, carrying out post-treatment to obtain N-Boc-N-methyl-4-aminostyrene. According to the method of the invention, raw materials are cheap and easilyavailable, reaction steps are simple, methylation and elimination reactions are completed at the same time through a one-pot reaction, yield is high, and cost is low.
Synthetic method AV - 45 intermediate (by machine translation)
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Paragraph 0073-0075, (2020/08/22)
The synthesis method of AV - 45 intermediate comprises the following steps: Step (1): The reaction of tert-butyl - N N-methyl -4 - vinylphenyl carbamate and 2 - bromo -5 - iodopyridine to obtain the intermediate A; step (2): condensation of the intermediate A and triethylene glycol to obtain a target compound. The synthesis method of the (E)-tert-butyl -4 - (2 - (6 - (2 - (2 -hydroxyethoxy) ethoxy) pyridin 2 -3 -yl) phenyl (meth) carbamate is improved, the reaction steps are few, and the intermediate and the target compound prepared from the route can be directly purified through recrystallization. (by machine translation)
68Ga-Bivalent Polypegylated Styrylpyridine Conjugates for Imaging Aβ Plaques in Cerebral Amyloid Angiopathy
Zha, Zhihao,Song, Jin,Choi, Seok Rye,Wu, Zehui,Ploessl, Karl,Smith, Megan,Kung, Hank
, p. 1314 - 1323 (2016/06/09)
Aβ plaques deposited on blood vessels are associated with cerebral amyloid angiopathy (CAA). In an effort to selectively map these Aβ plaques, we are reporting a new series of 68Ga labeled styrylpyridine derivatives with high molecular weights. In vitro binding to Aβ plaques in post-mortem Alzheimer's disease (AD) brain tissue showed that these 68Ga labeled bivalent styrylpyridines displayed good affinities and specificity (Ki 68Ga complexes to Aβ plaques. Biodistribution studies in normal mice showed very low initial brain uptakes (68Ga labeled bivalent styrylpyridines may be promising candidates as PET imaging radiotracers for detecting CAA.
Multidentate 18F-polypegylated styrylpyridines As imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA)
Zha, Zhihao,Choi, Seok Rye,Ploessl, Karl,Lieberman, Brian P.,Qu, Wenchao,Hefti, Franz,Mintun, Mark,Skovronsky, Daniel,Kung, Hank F.
, p. 8085 - 8098 (2012/01/13)
β-Amyloid plaques (Aβ plaques) in the brain are associated with cerebral amyloid angiopathy (CAA). Imaging agents that could target the Aβ plaques in the living human brain would be potentially valuable as biomarkers in patients with CAA. A new series of 18F styrylpyridine derivatives with high molecular weights for selectively targeting Aβ plaques in the blood vessels of the brain but excluded from the brain parenchyma is reported. The styrylpyridine derivatives, 8a-c, display high binding affinities and specificity to Aβ plaques (Ki = 2.87, 3.24, and 7.71 nM, respectively). In vitro autoradiography of [18F]8a shows labeling of β-amyloid plaques associated with blood vessel walls in human brain sections of subjects with CAA and also in the tissue of AD brain sections. The results suggest that [18F]8a may be a useful PET imaging agent for selectively detecting Aβ plaques associated with cerebral vessels in the living human brain.
SYNTHESIS OF 18F-RADIOLABELED STYRYLPYRIDINES FROM TOSYLATE PRECURSORS AND STABLE PHARMACEUTICAL COMPOSITIONS THEREOF
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, (2010/07/10)
The present invention relates to methods of synthesizing 18F-radiolabeled styrylpyridine and its tosylate precursor. The present invention further relates to stable pharmaceutical compositions comprising 18F-radiolabeled styrylpyridine.
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques
Qu, Wenchao,Kung, Mei-Ping,Hou, Catherine,Benedum, Tyler E.,Kung, Hank F.
, p. 2157 - 2165 (2008/02/05)
We report a series of radioiodinated styrylpyridines as single photon emission computed tomography probes for imaging Aβ plaques in the brain of patients with Alzheimer's disease (AD). In vitro binding showed that all of the styrylpyridines displayed very good binding affinities in postmortem AD brain homogenates (Ki = 3.6 to 15.5 nM). No-carrier-added samples of 13a, 13b, 16a, 16b, and 16e (radioiodinated with 125I) were successfully prepared. The in vivo biodistribution in normal mice, at 2 min after injection, showed excellent initial brain penetrations (4.03, 6.22, 5.43, and 8.04% dose/g for [125I]13a, 13b, 16a, and 16b, respectively). Furthermore, in vitro autoradiography of AD brain sections showed that the high binding signal was specifically due to the presence of Aβ plaques. Taken together, these results strongly suggest that these styrylpyridines are useful for imaging Aβ plaques in the living human brain.