301232-43-9Relevant articles and documents
Ni-Catalyzed β-Alkylation of Cyclopropanol-Derived Homoenolates
Mills, L. Reginald,Zhou, Cuihan,Fung, Emily,Rousseaux, Sophie A. L.
, p. 8805 - 8809 (2019/11/03)
Metal homoenolates are valuable synthetic intermediates which provide access to β-functionalized ketones. In this report, we disclose a Ni-catalyzed β-alkylation reaction of cyclopropanol-derived homoenolates using redox-active N-hydroxyphthalimide (NHPI) esters as the alkylating reagents. The reaction is compatible with 1°, 2°, and 3° NHPI esters. Mechanistic studies imply radical activation of the NHPI ester and 2e β-carbon elimination occurring on the cyclopropanol.
Quinoline derivatives as neurokinin receptor antagonists
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Page/Page column 33, (2009/04/24)
The present invention relates to substituted quinoline hydrazides of Formula (I): wherein R1, R2, R3, R4, R5, X, Y and Z are defined herein, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-2 and/or neurokinin-3 (NK-3) receptors. These compounds can thus be used in methods of treatment to suppress and treat such disorders.
N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II
Elliott, Jason M.,Carling, Robert W.,Chicchi, Gary G.,Crawforth, James,Hutson, Peter H.,Jones, A. Brian,Kelly, Sarah,Marwood, Rose,Meneses-Lorente, Georgina,Mezzogori, Elena,Murray, Fraser,Rigby, Michael,Royo, Inmaculada,Russell, Michael G.N.,Shaw, Duncan,Sohal, Bindi,Tsao, Kwei Lan,Williams, Brian
, p. 5752 - 5756 (2007/10/03)
Introduction of selected amine containing side chains into the 3-position of N′,2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted hPXR activation. Introduction of a fluorine at the 8-position is necessary to minimize unwanted hIKr affinity and a piperazine N-tert-butyl group is necessary for metabolic stability. The lead compound (8m) occupies receptors within the CNS following oral dosing (Occ90 7 mg/kg po; plasma Occ90 0.4 μM) and has good selectivity and excellent PK properties.