Li Zhang, Chao Wang, Jian Han, Zhi-Bin Huang^*（黄志斌）, 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

J. Org. Chem., 2016, 81 (12), pp 5256–5262

Pd-catalyzed regioselective coupling of β-C(sp²)–H bonds in aromatic amines protected by oxalyl amide with carbon monoxide is reported. The reaction could tolerate various functional groups and could afford good to excellent yields of the corresponding 3,4-dihydroisoquinolinone derivatives. Remarkably, it could also tolerate β-arylethylamino acid and thiopheneethylamine derivatives, thus showing their potential for producing several important units for bioactive compound synthesis.

链接：http://pubs.acs.org/doi/abs/10.1021/acs.joc.6b00932