A novel tandem reaction, which transforms N-(4,4-diethoxybutyl)imines to 3-arylidene-1-pyrrolines via intramolecular Mannich reaction/[1,3]-sigmatropic rearrangement of the aryl fragment is described.

2‐(Hetero)arylpyrrolidine fragment is found in a diverse array of biologically active molecules, both natural and unnatural. In recent years, a substantial increase in number of approved drugs featuring this scaffold is observed. Developing methods for the synthesis of such compounds has been essential for making progress in this field. Most of these methods require usage of metal catalysts and introduce additional chemical steps to obtain appropriately substituted starting compounds. This microreview details the one‐pot approach for the synthesis of pyrrolidine derivatives possessing (hetero)aromatic substituent at the second position of pyrrolidine ring based on usage of readily available N‐substituted 4,4‐diethoxybutan‐1‐amines and (hetero)aromatics as starting compounds and Bronsted acids as catalysts.

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