Nickel-Catalyzed Direct C (sp3)–H
Arylation of Aliphatic Amides with Thiophenes

Wang, Xie; Zhu, Longzhi; Chen, Sihai; Xu, Xinhua; Au, Chak-Tong; Qiu, Renhua

doi:10.1021/acs.orglett.5b02572.s001

ol5b02572_si_001.pdf (6.78 MB)

Nickel-Catalyzed Direct C (sp³)–H Arylation of Aliphatic Amides with Thiophenes

journal contribution

posted on 2015-11-06, 00:00 authored by Xie Wang, Longzhi Zhu, Sihai Chen, Xinhua Xu, Chak-Tong Au, Renhua Qiu

Nickel-catalyzed heteroarylation of the inactive methyl C(sp³)–H bond of aliphatic amide with heteroarenes is described. The method takes advantage of chelation assistance by an 8-aminoquinolinyl moiety. The synthetic reaction has good tolerance toward functional groups, and it can be used in the construction of various kinds of alkyl-substituted heteroarenes.