- Spiro(imidazo[1,2-a]pyrano[2,3-c]pyridine-9-indenes) as inhibitors of gastric acid secretion
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Asymmetric and symmetric spiro(imidazo[1,2-a]pyrano[2,3-c]pyridine-9-indenes) were prepared using a synthetic approach that comprised a cross-metathesis reaction and an acid-catalyzed cycloisomerisation as key steps. The target compounds constitute potent inhibitors of the gastric proton pump enzyme with inhibitory activity comparable to potassium-competitive acid blockers (P-CABs) belonging to the known 9-aryl-7H-8,9-dihydropyrano[2,3-c]imidazo[1,2-a]pyridine series. Spiro(imidazo[1,2-a]pyrano[2,3-c]pyridine-9,2′-indenes) represent the first example for P-CABs, in which the distance between the heterocyclic scaffold and the aryl residue has been modified, and are promising candidates for further development as anti-ulcer drugs.
- Palmer, Andreas Marc,Chrismann, Sandra,Muench, Gabriela,Brehm, Christof,Zimmermann, Peter Jan,Buhr, Wilm,Senn-Bilfinger, Joerg,Feth, Martin Philipp,Simon, Wolfgang Alexander
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experimental part
p. 368 - 384
(2011/02/26)
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- Palladium-catalyzed carbonylative cyclization via trapping of acylpalladium derivatives with internal enolates. Its scope and factors affecting the C-to-O ratio
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The Pd-catalyzed carbonylative cyclization reaction involving ω-acyl-substituted acylpalladium derivatives can proceed via intramolecular trapping with either C- or O-enolates; the preferential formation of either 5- or 6-membered rings dictates the C-to-
- Negishi, El-Ichi,Coperet, Christophe,Sugihara, Takumichi,Shimoyama, Izumi,Zhang, Yantao,Wu, Guangzhong,Tour, James M.
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p. 425 - 436
(2007/10/02)
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