40759-46-4Relevant academic research and scientific papers
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: Trends across multiple chemical series
Nersesian, Diana L.,Black, Lawrence A.,Miller, Thomas R.,Vortherms, Timothy A.,Esbenshade, Timothy A.,Hancock, Arthur A.,Cowart, Marlon D.
, p. 355 - 359 (2008/04/03)
Structure-activity relationships (SAR) were analyzed within a library of diverse yet simple compounds prepared as histamine H3 antagonists. The libraries were constructed with a variety of low molecular weight pyrrolidines, selected from (R)-2-methylpyrrolidine, (S)-2-methylpyrrolidine, and pyrrolidine.
NEW OXABISPIDINE COMPOUNDS FOR THE TREATMENT OF CARDIAC ARRHYTHMIAS
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Page/Page column 86, (2010/11/27)
There is provided compounds of formula I, [Chemical formula should be inserted here. Please see paper copy] wherein R1 to R4 , R41 to R46 and Z have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias
The Structure and Function of Estrogens. XI. Synthesis of (+/-)-7(8->11α)abeo-Estradiol and its 9,11-Didehydro Derivative
Collins, David J.,Fallon, Gary D.,Skene, Colin E.
, p. 71 - 97 (2007/10/02)
Two approaches to the synthesis of (+/-)-7(8->11α)abeo-estra-1,3,5(10)triene-3,17β-diol (2a) from (+/-)-1β-t-butoxy-7aβ-methyl-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (11) were studied.A pathway involving 6-alkylation of (11) with 2-(3'-methoxyphenyl)ethyl halides or sulfonate esters was unsuccessful, but conjugate addition of 3-methoxybenzyl nucleophiles with (+/-)-1β-t-butoxy-7aβ-methyl-6-methylene-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (18), prepared from (11), led to (+/-)-1β-t-butoxy-6α--7aβ-methyl-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (10a).Acid-catalyzed cyclization of (10a) afforded (+/-)-17β-t-butoxy-3-methoxy-7(8->11)abeo-estra-1,3,5(10),9(11)-tetraene (29) which upon lithium/ammonia reduction in the presence of diphenylmethane gave (+/-)-17β-t-butoxy-3-methoxy-7(8->11α)abeo-estra-1,3,5(10)-triene (31).Deprotection of (31) and (29) afforded (+/-)-7(8->11α)abeo-estra-1,3,5(10)-triene-3,17β-diol (2a) and (+/-)-7(8->11)abeo-estra-1,3,5(10),9(11)-tetraene-3,17β-diol (32), respectively. Alternatively, reaction of (+/-)-1β-t-butoxy-7aβ-methyl-6-methylene-2,3,3aα,6,7,7a-hexahydro-1H-inden-5(4H)-one (18) with 3-methoxybenzyl phenyl sulfoxide (23a) gave (1RS,3'SR,2RS,3a'SR,7a'SR)-3'-t-butoxy-2-(3''-methoxyphenyl)-3a'-methyl-2',3',3a',4',7',7a'-hexahydrospiroinden>-6'(1'H)-one (26), reductive cleavage of which with lithium/ammonia afforded (10a). The relative stereochemistries of (31) and of the spiro cyclopropyl ketone intermediate (26) were established unambiguously by X-ray crystallography.
Benzothiazepine vasodilators having aralkyl substitution
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, (2008/06/13)
N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): STR1 for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators.
Synthesis and Pharmacological Studies of 4,4-Disubstituted Piperidines: A New Class of Compounds with Potent Analgesic Properties
Huegi, Bruno S.,Ebnoether, Anton M.,Rissi, Erwin,Gadient, Fulvio,Hauser, Daniel,et al.
, p. 42 - 50 (2007/10/02)
A series of 4,4-disubstituted piperidines has been synthesized and evaluated for analgesic activity.Several of these analogues show analgesic potency comparable to morphine in the mouse writhing and tail-flick tests.A number of compounds exhibit high affi
