Selective Cmath image[BOND]Csp Bond Cleavage: The Nitrogenation of Alkynes to Amides


  • Financial support from the National Basic Research Program of China (973 Program) (Grant No. 2009CB825300), the National Science Foundation of China (No. 21172006), and the Ph.D. Programs Foundation of the Ministry of Education of China (No. 20120001110013) are greatly appreciated. We thank Yizhi Yuan for reproducing the results of 4 f and 4 i in Table 3.


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Breakthrough: A novel catalyzed direct highly selective Cmath image[BOND]Csp bond functionalization of alkynes to amides has been developed. Nitrogenation is achieved by the highly selective Cmath image[BOND]Csp bond cleavage of aryl-substituted alkynes. The oxidant-free and mild conditions and wide substrate scope make this method very practical.