69883-78-9Relevant academic research and scientific papers
Process for the preparation of cyclic diketones
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Page/Page column 10-11, (2008/06/13)
The present invention relates to a process for the preparation of compounds of formula I wherein the substituents are as defined in claim 1, by conversion of a compound of formula II reaction of that compound with a compound of formula IV X—C(O)—Q ??(IV) wherein X is a leaving group, to form a compound of formula V and treatment of that compound in the presence of a base with catalytic amounts of cyanide ions.
Inotropic 2-arylimidazo[1,2-a]pyrimidines
Barraclough,Black,Cambridge,Capon,Cox,Firmin,Gerskowitch,Giles,Glen,Hill,Hull,Iyer,Kettle,King,Nobbs,Randall,Skone,Smith,Vine,et al.
, p. 207 - 217 (2007/10/02)
A series of 2-arylimidazo[1,2-a]pyrimidines has been prepared and evaluated for inotropic activity. Three of these heterocycles, ether 19, sulphide 21 and mesylate 24 displayed more potent inotropic effects in vitro than isomazole. The in vivo inotropic p
Safety-catch anchoring linkage for synthesis of peptide amides by Boc/Fmoc strategy
Patek,Lebl
, p. 3891 - 3894 (2007/10/02)
2-Methoxy-4,4'-bis(methylthio)benhydrylamine (10) and the corresponding disulfoxide were prepared and tested as a model amide protecting groups for their stability toward acidic conditions. Subsequently, the novel 4-[4,4'-bis(methylsulfinyl)-2-oxy-(9-fluorenylmethyloxycarbonyl) benzhydrylamino]butanoic acid (SCAL) handle (9) has been prepared and applied to solid-phase peptide synthesis of C-terminal peptide amide using both 9-fluorenylmethyloxycarbonyl (Fmoc) and tert-butyloxycarbonyl (Boc) groups for N(α)-amino protection.
Inotropic activity of heterocyclic analogues of isomazole
Barraclough, P.,Beams, R. M.,Black, J. W.,Cambridge, D.,Collard, D.,et al.
, p. 467 - 477 (2007/10/02)
Aryl-substituted benzimidazole, imidazopyridine, imidazopyrazine, imidazopyridazine, oxazolopyridine, purine, pyrollopyridine and thiazolopyridine derivatives have been prepared and evaluated as inotropic agents.Purine 8 and the 1H-imidazo- and pyridazines 9 and 10 proved to be of most interest, having similar in vivo inotropic potencies to sulmazole.The pKa's, protonation sites and lipophilicities for most heterocycles were determined experimentally and some of their electronic properties calculated.For a subset of active heterocycles a correlation was observed between in vitro inotropism and the charge density of the imidazo nitrogen adjacent to the electrostatic potential minimum.Structure-activity relationships are discussed in some detail.
Inotropic 'A' ring substituted sulmazole and isomazole analogues
Barraclough,Black,Cambridge,Collard,Firmin,Gerskowitch,Glen,Giles,Hill,Hull,Iyer,King,Kneen,Lindon,Nobbs,Randall,Shah,Smith,Vine,et al.
, p. 2231 - 2239 (2007/10/02)
A series of 'A' ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pK(A)'s, protonation sites, and log P values were measured for selected compounds and their electronic properties were calculated. No simple correlation between inotropic activity and pK(A), protonation site, or log P value was observed. However, in vitro inotropism did correlate with the calculated charge density of the 'B' ring imidazo nitrogen atom. The 6-position of sulmazole appeared to be the most tolerant toward substituents, th 6-amino derivative 7 being a more potent inotrope than sulmazole itself. 4-Methoxyisomazole 13 had comparable in vivo inotropic properties to those of isomazole.
