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Issue 26, 2013
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Trisubstitution of pyridine through sequential and regioselective palladium cross-coupling reactions affording analogs of known GPR54 antagonists

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Abstract

Because of their large spectrum of applications, poly-functionalized pyridines remain an attractive challenge in modern organic chemistry. We describe the poly-functionalization of halopyridines through a series of sequential and regioselective palladium-catalyzed cross-coupling reactions (Suzuki–Miyaura, Sonogashira and Buchwald–Hartwig reactions). This strategy was applied to the synthesis of several analogs of single non-peptidic known GPR54 antagonists.

Graphical abstract: Trisubstitution of pyridine through sequential and regioselective palladium cross-coupling reactions affording analogs of known GPR54 antagonists

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Article information


Submitted
30 Jan 2013
Accepted
02 May 2013
First published
02 May 2013

RSC Adv., 2013,3, 10296-10300
Article type
Paper

Trisubstitution of pyridine through sequential and regioselective palladium cross-coupling reactions affording analogs of known GPR54 antagonists

C. Doebelin, P. Wagner, I. Bertin, F. Simonin, M. Schmitt, F. Bihel and J. Bourguignon, RSC Adv., 2013, 3, 10296
DOI: 10.1039/C3RA41985A

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