Metal‐ and Solvent‐free, Methodical <i>In situ</i> Activation of Alkynes to Access Imidazo[1,2‐<i>a</i>]pyrazines from 2‐Cyanoimidazoles

Abstract An efficient one‐pot, metal and solvent ‐ free synthetic method has been developed to access multisubstituted imidazo[1,2‐ a ]pyrazines from 1‐(3‐alkynyl)‐1 H ‐imidazole‐2‐carbonitriles achieving in excellent yields. This organic transformation involves the formation of two new C−N bonds via the imine‐induced in situ activation of the alkyne, followed by 6‐exo‐dig cyclization and subsequent aromatization. The process is compatible with complex natural products and drug intermediates and is distinguished by its high atom economy, wide substrate applicability under appropriate reaction conditions.