29194-89-6Relevant academic research and scientific papers
Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands
Lazewska, Dorota,Kuder, Kamil,Ligneau, Xavier,Camelin, Jean-Claude,Schunack, Walter,Stark, Holger,Kiec-Kononowicz, Katarzyna
experimental part, p. 3037 - 3042 (2009/09/30)
Synthesis and biological activities of a series of homo- or substituted piperidine unsymmetrical diethers are described. The novel compounds were evaluated for histamine H3 receptor binding affinities at recombinant human H3 receptor
Nucleophilic addition to iminium ethers in the preparation of functionalized N-alkyl heterocycles
Fenster, Erik,Smith, Brenton T.,Gracias, Vijaya,Milligan, Gregory L.,Aube, Jeffrey
, p. 201 - 205 (2008/09/16)
(Chemical Equation Presented) Bicyclic iminium ethers can be synthesized by the reactions of ketones with hydroxyalkyl azides. These cationic species react with a variety of nucleophiles via two possible pathways. The initially formed, kinetic product arises from direct addition to the iminium carbon in the substrate. In some cases, the initial adduct reverts to the starting iminium ether and the ultimate product arises from nucleophilic displacement at the O-alkyl group to afford the terminally functionalized N-substituted amide. The behavior of a range of nucleophiles was studied by using several iminium ethers. In general, the relevant pathway could be identified by characterization of the product formed. For hydroxide addition, which can afford only one product regardless of mechanism, the reaction was shown to arise by the kinetic pathway, using 18O-labeled hydroxide. A one-pot synthesis of functionalized lactams entailing treatment of ketones first with hydroxyalkyl azides followed by nucleophilic addition was also developed.
Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
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Page/Page column 51, (2008/06/13)
The invention relates to tetrahydronaphthyridine derivatives having formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said tetrahydronaphthyridine derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Synthesis and structure-activity relationships of cetiedil analogues as blockers of the Ca2+-activated K+ permeability of erythrocytes
Roxburgh,Ganellin,Athmani,Bisi,Quaglia,Benton,Shiner,Malik-Hall,Haylett,Jenkinson
, p. 3244 - 3253 (2007/10/03)
Cetiedil, [2-cyclohexyl-2-(3-thienyl)ethanoic acid 2-(hexahydro-1H-azepin-1-yl)ethyl ester], which blocks the intermediate calcium-activated potassium ion permeability (IKCa) in red blood cells, was used as a lead for investigating structure-ac
HYDROBORATION OF N-ALLYL DERIVATIVES OF PYRROLIDINE, PIPERIDINE, HEXAHYDROAZEPINE AND MORPHOLINE
Ferles, Miloslav,Kafka, Stanislav
, p. 2150 - 2156 (2007/10/02)
Heating of allyl derivatives I with triethylamine-borane gave spirocyclical amine-boranes II, which were hydrolysed with hydrochloric acid to hydrochlorides of aminoboronic acids, III.Oxidation of these hydrochlorides produced aminoalcohols IV.
