952734-38-2Relevant academic research and scientific papers
AMIDE DERIVATIVES COMPRISING HETEROCYCLOALKYL RING
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Paragraph 0267-0269, (2020/05/20)
PROBLEM TO BE SOLVED: To provide compounds or pharmacologically acceptable salts thereof that have excellent EP300 and/or CREBBP histone acetyltransferase inhibitory activity. SOLUTION: The invention provides compounds represented by the formula (1) in the figure or pharmacologically acceptable salts thereof. (In the formula (1), ring Q1, ring Q2, ring Q3, X and L are as defined in the specification.) SELECTED DRAWING: None COPYRIGHT: (C)2020,JPO&INPIT
Direct C3-Arylation of 2 H-Indazole Derivatives with Aryl Bromides by using Low Loading of a Phosphine-free Palladium Catalyst
Belkessam, Fatma,Aidene, Mohand,Soulé, Jean-Fran?ois,Doucet, Henri
, p. 2239 - 2249 (2017/06/27)
The palladium-catalyzed direct arylation of 2 H-indazoles with aryl bromides for the preparation of 3-aryl-2 H-indazoles was found to proceed in high yields when using only 0.5–0.1 mol % Pd(OAc)2 catalyst and KOAc as inexpensive base. A wide variety of electron-deficient and electron-rich aryl bromides and also heteroaryl bromides has been successfully employed. Both electron-withdrawing and electron-donating substituents on the 2 H-indazoles are also tolerated. Moreover, the reaction can be performed in the “green” solvent cyclopentyl methyl ether.
Process for the Preparation of Indazolyl Ureas that Inhibit Vanilloid Subtype1 (VR1) Receptors
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Page/Page column 12, (2008/06/13)
The present invention relates to a process of preparing indazolyl ureas that are useful as antagonists of the vanilloid receptor subtype 1 (VR1).
New practical synthesis of indazoles via condensation of o-fluorobenzaldehydes and their O-methyloximes with hydrazine
Lukin, Kirill,Hsu, Margaret C.,Fernando, Dilinie,Leanna, M. Robert
, p. 8166 - 8172 (2007/10/03)
The reaction of o-fluorobenzaldehydes and their O-methyloximes with hydrazine has been developed as a new practical synthesis of indazoles. Utilization of the methyloxime derivatives of benzaldehydes (in the form of the major E-isomers) in this condensation effectively eliminated a competitive Wolf-Kishner reduction to fluorotoluenes, which was observed in the direct preparations of indazoles from aldehydes. Reaction of Z-isomers of methyloximes with hydrazine resulted in the formation of 3-aminoindazoles via a benzonitrile intermediate.
