Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Current Topics: Communications to the Editor
Palladium-Catalyzed C–H Heteroarylation of 2,5-Disubstituted Imidazoles
Takaya TogoYouhei SohmaYoichiro KuninobuMotomu Kanai
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2019 Volume 67 Issue 3 Pages 196-198

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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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© 2019 The Pharmaceutical Society of Japan
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