| Summary: | <i>N</i>-dealkylation, the removal of an <i>N</i>-alkyl group from an amine, is an important chemical transformation which provides routes for the synthesis of a wide range of pharmaceuticals, agrochemicals, bulk and fine chemicals. <i>N</i>-dealkylation of amines is also an important in vivo metabolic pathway in the metabolism of xenobiotics. Identification and synthesis of drug metabolites such as <i>N</i>-dealkylated metabolites are necessary throughout all phases of drug development studies. In this review, different approaches for the <i>N</i>-dealkylation of amines including chemical, catalytic, electrochemical, photochemical and enzymatic methods will be discussed.
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