Copper promoted aerobic oxidative c(sp³)-c(sp³) bond cleavage of n-(2-(pyridin-2-yl)-ethyl)anilines

A strategy of aerobic oxidative C(sp³)-C(sp³) bond cleavage of N-ethylaniline derivatives bearing azaarenes for the synthesis of N-aryl formamides has been developed. This approach was carried out smoothly with the CuI/TEMPO/air system to give N-aryl formamides in yields of 50-90%. With this methodology, a mutagenically active compound was constructed in 90% yield. Moreover, the reaction also provided a one-pot synthetic tool for accessing a promoter of hematopoietic stem cells by difunctionalization in 61% yield.