Brasche, Gordon
Buchwald, Stephen L

C–H Functionalization/C–N Bond Formation: Copper-Catalyzed Synthesis of Benzimidazoles from Amidines

“,
Angew. Chem. Int. Ed.
,
2008
,
47
(
10
)
,
1932-1934
.
Abstract

Benzimidazoles are synthesized from amidines through a copper-catalyzed C–H functionalization/C–N bond-forming process. The method tolerates a broad range of functional groups and provides the benzimidazoles in up to 89 % yield. Best results are obtained by using 15 mol % Cu(OAc)2, 2–5 equivalents of HOAc as additive, and oxygen as the stoichiometric reoxidant.