94567-78-9Relevant academic research and scientific papers
Gold-catalyzed hydroarylation of allenes: A highly regioselective carbon-carbon bond formation producing six-membered rings
Watanabe, Toshiaki,Oishi, Shinya,Fujii, Nobutaka,Ohno, Hiroaki
, p. 4821 - 4824 (2007)
(Chemical Equation Presented) Gold-catalyzed intramolecular hydroarylation of allenic anilines and phenols offers an efficient route to dihydroquinoline and chromene derivatives under mild reaction conditions. The hydroarylation takes place at the terminal or central allenic carbon depending on the substrate structure, leading to a highly selective formation of six-membered rings.
SUBSTITUENT EFFECTS ON THE REDUCTIONS OF QUINOLINE-N-BORANES
Blackburn, Brent K.,Frysinger, John F.,Minter, David E.
, p. 4913 - 4916 (1984)
Reductions of 2-substituted quinoline-N-boranes by sodium bis-(2-methoxyethoxy)aluminum dihydride lead to 1,2,3,4-tetrahydroquinolines by hydride attack at C-4 and subsequent reduction of the resulting enamine.
AMINO PYRIMIDINE COMPOUND FOR INHIBITING PROTEIN TYROSINE KINASE ACTIVITY
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Paragraph 0422; 0423, (2019/06/07)
An amino pyrimidine compound for inhibiting protein tyrosine kinase activity, a pharmaceutical composition thereof, preparation therefor, and an application thereof. Specifically, an amino pyrimidine compound represented by formula (I), R1, R2, L, Y, R6, W, A, m, and n being defined in the specification, and a pharmaceutically acceptable salt, a stereoisomer, a solvent compound, a hydrate, a polymorphism, a prodrug, or an isotope variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases such as cell proliferative diseases, cancers, and immune diseases.
Design, synthesis and structure-activity relationship of novel tricyclic benzimidazolone derivatives as potent 18 kDa translocator protein (TSPO) ligands
Fukaya, Takayuki,Kodo, Toru,Ishiyama, Takeo,Nishikawa, Hiroyuki,Baba, Satoko,Masumoto, Shuji
, p. 1257 - 1267 (2013/03/28)
The 18 kDa translocator protein (TSPO) was identified as a discrete receptor for diazepam (1). Since TSPO in the central nervous system (CNS) is believed to regulate neurosteroids biosynthesis, selective TSPO ligands are expected to be useful in the treatment of psychiatric disorders. We synthesized three novel tricyclic benzimidazolone derivatives, and selected the dihydroimidazoquinolinone derivative 27 as a lead TSPO ligand. Study of the structure-activity relationship (SAR) of dihydroimidazoquinolinone derivatives revealed compounds with potent affinity for TSPO (subnanomolar Ki values), but poor metabolic stability. The optimization of these compounds led to compound 48 with potent affinity for TSPO and good in vitro PK profile.
Synthesis of diverse 2,3-dihydroindoles, 1,2,3,4-tetrahydroquinolines, and benzo-fused azepines by formal radical cyclization onto aromatic rings
Clive, Derrick L. J.,Peng, Jianbiao,Fletcher, Stephen P.,Ziffle, Vincent E.,Wingert, David
, p. 2330 - 2344 (2008/09/19)
(Chemical Equation Presented) 2,3-Dihydroindoles, 1,2,3,4- tetrahydroquinolines, and 2,3,4,5-tetrahydrobenzo[b]azepines are available by a process that represents formal radical cyclization onto aromatic rings. Optically pure benzo-fused heterocycles are also accessible by this method. p-Iodophenols, especially those with the phenolic oxygen protected as a MOM-ether, can be coupled with amino alcohols to produce N-aryl amino alcohols, which can be converted into the corresponding alkyl iodides in which the nitrogen is protected as a carbamate. These compounds give cross-conjugated ketones after removal of the phenolic protecting group and oxidation with PhI(OAc)2 in the presence of MeOH. The ketones undergo 5-, 6- or 7-exo-trigonal radical cyclization, and then exposure to acid, or sequential treatment with a Grignard reagent and then acid, effects rearomatization to produce the benzo-fused nitrogen heterocycles.
NOVEL HETEROCYCLIC COMPOUND
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Page/Page column 28, (2010/11/24)
A drug having a high affinity for benzodiazepine ω3 receptors and showing curative and preventive effects for anxiety and depression, which comprises as the active ingredient, for example, a compound of the formula (1): wherein R1 an
