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.

中文翻译：

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N-（2-（吡啶-2-基）-乙基）苯胺的铜促进的好氧氧化C（sp3）-C（sp3）键裂解。

已开发出一种策略，对带有氮杂芳烃的N-乙基苯胺衍生物进行好氧氧化C（sp3）-C（sp3）键裂解，以合成N-芳基甲酰胺。该方法在CuI / TEMPO /空气系统中顺利进行，得到N-芳基甲酰胺，收率为50-90％。使用这种方法，诱变活性化合物的产率为90％。而且，该反应还提供了一种单罐合成工具，用于通过双官能化以61％的产率访问造血干细胞的启动子。