Abstract
AbstractIn this paper, we report a new and facile protocol for anti‐Markovnikov hydroamination of vinyl pyridines under mild condition. In the presence of organic peroxide, pyridylethylation of a wide variety of aryl/alkyl amines with different substituent and electronic characteristics by intermolecular anti‐Markovnikov hydroamination was successfully carried out. Furthermore, moderate to excellent yields were obtained along with high selectivity through condition optimization. The highest yield of target product can reach 93 % in gram‐scale reaction. On the basis, we proposed a kind of aza‐Michael‐type free radical addition mechanism, which was well supported by deuterium labeling studies and reference experiments.
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