Rhodium(III)-Catalyzed Oxidative C–H/C–H Cross-Coupling of Heteroarenes and Masked Benzylamines

Jundie Hu, Guobao Li, Chunchen Yuan, Zhi-Bin Huang, Da-Qing Shi^*（史达清）, and Yingsheng Zhao^*（赵应声）

Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, China

Org. Lett., 2016, 18 (23), pp 5998–6001

The first example of oxidative C–H/C–H cross-coupling of oxalyl amide-protected benzylamines and various heteroarenes in the presence of a rhodium(III) catalyst has been developed. The route provides a means of synthesizing ortho-heteroarylated benzylamines. The methodology presents broad substrate scope, great functional group tolerance, and good to excellent yields in the synthesis of substituted benzylamines. The study also reveals that the thienoisoquinoline derivatives can be accessed through the intramolecular amination of thiophenyl-substituted benzylamines with palladium(II).

链接：http://pubs.acs.org/doi/abs/10.1021/acs.orglett.6b02773