Rhodium(III)-Catalyzed Oxidative Cross-Coupling of Unreactive C(sp3)-H Bonds with C(sp2)-H Bonds
1Key Laboratory of Green Chemistry and Technology of Ministry of Education, College of Chemistry, Sichuan University , 29 Wangjiang Road, Chengdu 610064, P.R. China.
Abstract:
The development of the oxidative cross-coupling of unreactive C(sp3)-H bonds with (hetero)arene C(sp2)-H bonds is considerably appealing, yet conceptually and practically challenging. Here, we disclose the rhodium-catalyzed oxidative heteroarylation of unactivated C(sp3)-H bonds with heteroarene C(sp2)-H bonds. This method provides a step-economic route to β-heteroarylated 2-ethylpyridine derivatives, which exhibits relatively broad substrate scope, high tolerance level of sensitive functional groups, and high selectivity. The protocol can also be extended to the coupling reaction between 8-methylquinoline derivatives and heteroarenes.
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