2019
DOI: 10.1248/cpb.c18-00586
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Palladium-Catalyzed C–H Heteroarylation of 2,5-Disubstituted Imidazoles

Abstract: We developed a palladium-catalyzed C-H N-heteroarylation of N-protected-2,5-disubstituted imidazoles at the C4position using N-heteroaryl halides as a coupling partner. Intensive reaction condition screening led us to identify fluorinated bathophenanthroline 7 as the optimum ligand for the palladium catalyst. This reaction will enhance lead optimization of drug candidates by facilitating the synthesis of heterobiaryl compounds containing an imidazole ring.

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