153747-97-8Relevant articles and documents
Selective Amination of Polyhalopyridines Catalyzed by a Palladium-Xantphos Complex
Ji, Jianguo,Li, Tao,Bunnelle, William H.
, p. 4611 - 4614 (2003)
(Matrix presented) Amination of 5-bromo-2-chloropyridine (1a) catalyzed by a palladium-Xantphos complex predominately gives 5-amino-2-chloropyridine product 3a in 96% isolated yield and excellent chemoselectivity (3a/4a = 97:3). Amination of 2,5-dibromopyridine (11) under the same conditions exclusively affords 2-amino-5-bromopyridine 4a.
OGA INHIBITOR COMPOUNDS
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Page/Page column 43; 48, (2021/06/26)
The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations; or alpha synucleinopathies, in particular Parkinson's disease, dementia due to Parkinson's (or neurocognitive disorder due to Parkinson's disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher's disease.
3-substituent-5-(substituted aryl)-7-azaindole derivative and application thereof
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Paragraph 0033; 0038-0040, (2021/09/01)
The invention discloses a 3-substituent-5-(substituted aryl)-7-azaindole derivative and application thereof. The structural formula of the 3-substituent-5-(substituted aryl)-7-azaindole derivative is shown in the specification, and the 3-substituent-5-(substituted aryl)-7-azaindole derivative has obvious anti-coronavirus activity. In-vitro binding experiments show that the 3-substituent-5-(substituted aryl)-7-azaindole derivative disclosed by the invention generally has relatively strong affinity with a drug target 3CLPro protease of coronavirus, can effectively inhibit the activity of the 3CLPro protease, and is a small molecular ligand for targeted inhibition of 3CLPro.