1234208-02-6Relevant articles and documents
Synthetic method AV - 45 intermediate (by machine translation)
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Paragraph 0053-0063, (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)
Facile synthesis of TEG-substituted 4-(N-methyl-N-Boc-amino)styrylpyridine and PET imaging agent [F]florbetapir ([F]AV-45)
Yao, Tuo,Li, Zhi
, p. 422 - 427 (2018/02/06)
Triethylene glycol-substituted 4-(N-methyl-N-Boc-amino)styrylpyridine which can serve as key precursor for many monodentate and multidentate imaging agents for Aβ plaques in human brain has been readily synthesized with cost-effective starting materials. The important non-radioactive monodentate positron emission tomography agent [F]florbetapir ([F]AV-45) has also been prepared by our new method.
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.
Synthesis of TEG-Substituted 4-(N-Methyl-N-Boc-amino)styrylpyridine as Key Precursor for Monodentate and Multidentate Imaging Agents for A β Plaques
Li, Zhi,Liu, Bo,Duan, Wubiao,Zhu, Lin
, p. 2740 - 2747 (2015/12/18)
Triethylene glycol (TEG)-substituted 4-(N-methyl-N-Boc-amino)styrylpyridine, which can serve as key precursor for many monodentate and multidentate imaging agents for Aβ plaques in the human brain, has been readily synthesized with cheap starting materials. Our new method could be employed for mass production of monodentate imaging agent AV-45 and other multidentate imaging agents.
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.
experimental part, 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.