A Palladium-Catalysed Urea Arylation Route to a CRF1 Receptor Antagonist

Popkin, Matthew E.; Bellingham, Richard K.; Hayes, Jerome F.

doi:10.1055/s-2006-950276

Cited by 7 publications

(3 citation statements)

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“…[195] GlaxoSmithKline scientists used a bisannulation process in a new approach to the potent CRF 1 antagonist GW808990 (Scheme 39). [196] The chelating ligand DPEPhos was also found to be capable of mediating the reaction, but in significantly lower yield than observed with MePhos.…”

Section: Applications In Pharmaceutical Synthesismentioning

confidence: 92%

Biaryl Phosphane Ligands in Palladium‐Catalyzed Amination

2008

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Palladium-catalyzed amination of aryl halides has undergone rapid development in the last 12 years. This has been largely driven by implementation of new classes of ligands. Biaryl phosphines have proven to provide especially active catalysts in this context. This review discusses the applications that these catalysts have found in C-N cross-coupling in heterocycle synthesis, pharmaceuticals, materials science and natural product synthesis.

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Section: Applications In Pharmaceutical Synthesismentioning

confidence: 92%

Biaryl Phosphane Ligands in Palladium‐Catalyzed Amination

2008

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“…[194] Dieser von Buchwald [195] Wissenschaftler von GlaxoSmithKline nutzten eine doppelte Anellierung als neuen Zugang zu dem CRF 1 -Antagonisten GW808990 (Schema 39). [196] Auch der Chelatligand DPEPhos förderte die Reaktion, resultierte jedoch in einer erheblich geringeren Ausbeute als MePhos.…”

Section: Anwendungen In Der Wirkstoffsyntheseunclassified

Biarylphosphanliganden in der palladiumkatalysierten Aminierung

2008

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In den vergangenen 12 Jahren erfuhr die palladiumkatalysierte Aminierung von Arylhalogeniden eine rasche Entwicklung, die durch die Einführung neuer Ligandenklassen vorangetrieben wurde. Biarylphosphane liefern in diesem Zusammenhang besonders reaktive Katalysatoren. Dieser Aufsatz behandelt Anwendungen solcher Katalysatoren zur C‐N‐Kreuzkupplung in der Synthese von Heterocyclen und Pharmazeutika, in den Materialwissenschaften und in der Naturstoffsynthese.

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“…Notably, the 1-(piperidin-4-yl)-1 H -imidazo[4,5- b ]pyridin-2(3 H )-one core of Telcagepant is such a privileged structure that it constitutes the backbone of more than 1000 unique small molecule antagonist of CGRP receptors. 13 Other prominent examples of pharmacologically relevant derivatives of imidazo[4,5- b ]pyridin-2-ones examples include WO2011021678A1 (p38 MAPK inhibitor) 14 and GW808990 (a CRF1 receptor antagonist). 15…”

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confidence: 99%