Direct base‐mediated amination of aryl halides with aliphatic tertiary amines via an aryne intermediate was developed under transition‐metal‐free conditions. This operationally simple C–N bond‐coupling protocol could tolerate a variety of functionalized aryl halides as well as several aliphatic tertiary amines. Moreover, this environmentally benign process provides a new strategy for direct C–N bond formation.
Aliphatic tertiary amines can exhibit considerable nucleophilicity. The combination of aryl halides and aliphatic tertiary amines provides efficient access to biochemically important aromatic amines. It is noteworthy that this direct amination takes place in the absence of transition metal catalysts.
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