Abstract

Abstractα‐ and β‐Functionalized amines are two classes of important compounds, whose structural units are widely present in approved drugs. The hydrofunctionalization of enamides is the most direct and efficient method for constructing these two types of compounds. Regioselectivity is the focus of this conversion, and is largely influenced by the catalytic mode. Therefore, to selectively synthesize α‐ or β‐functionalized amines, the progress in the catalytic hydrofunctionalization of enamides over the past decade is reviewed, and the catalytic pathways for this process discussed in detail. This account aims to objectively evaluate the effects of various catalytic pathways on the regioselectivity of hydrofunctionalization, to provide a new perspective on the selection of catalytic methods and the design of catalytic pathways for the selective synthesis of α‐ or β‐functionalized amines.

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