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Updated: Feb 4, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Palladium-Catalyzed C-H Heteroarylation of 2,5-Disubstituted Imidazoles
Takaya Togo1, Youhei Sohma1, Yoichiro Kuninobu2
1Graduate School of Pharmaceutical Sciences, The University of Tokyo.
Abstract:
We developed a palladium-catalyzed C-H N-heteroarylation of N-protected-2,5-disubstituted imidazoles at the C4-position 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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