Abstract

1,2‐Aziridinyl propargylic amines have been obtained through a zinc‐catalyzed multicomponent reaction. This process relies on the dimeric amino aldehyde assembly orchestrating the intramolecular 1,2‐alkyne addition to an iminium ion. The resulting products can be readily elaborated through regioselective aziridine ring opening. A catalytic cycle and stereochemical rationale for the highly anti‐selective alkyne addition is proposed.

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