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A straightforward strategy was developed for the arylation and olefination at the C5-position of the N-(alkyl)pyrimidin-2-amine core with readily available aryl halides and alkenes, respectively. This approach was highly regioselective, and the transformation was achieved based on two different (Pd(II)/Pd(IV)) and (Pd(0)/Pd(II)) catalytic cycles.

Graphical abstract: Palladium-catalyzed remote C–H functionalization of 2-aminopyrimidines

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