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.
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