Abstract

AbstractThe propargylamine motif is not only prevalent in a wide variety of pharmaceuticals and other biologically active compounds but also utilized as a versatile building block in organic synthesis. Among the various methods for the synthesis of propargylamine derivatives, A3‐coupling represents one of the most general and attractive routes, since it offers the possibility for the construction of complex molecules from simple starting materials (amines, aldehydes, and alkynes) in one‐step with high atom economy. However, the use of volatile alkynes is the main disadvantage of this reaction. Recently, alkynyl carboxylic acids were successfully used as easily accessible and high stable surrogates for alkynes (via in situ decarboxylation) in A3‐coupling reactions. This Focus‐Review aims to give an overview of the decarboxylative A3‐coupling reactions by hoping that it will be beneficial to elicit further research in this appealing research arena. A special emphasis is placed on mechanistic aspect of reactions which may allow possible new insights into catalyst improvement.

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