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An acid-catalyzed multicomponent tandem double cyclization protocol has been developed for the synthesis of polyfunctional 4,9-dihydropyrrolo[2,1-b]quinazolines from simple and readily available arylglyoxal monohydrates, 2-aminobenzylamine, and trans-β-nitrostyrenes. This practical and metal-free reaction proceeds through an imine formation/cyclization/Michael addition/Henry cyclization protocol, resulting in the construction of four new bonds and two ring moieties directly in one pot.

Simple, readily available starting materials are used for the preparation of the desired alkaloid scaffold under metal-free conditions A) or B).

A novel strategy has been developed for the direct synthesis of 2-aroyl-3-hydroxy-4-iodonaphthalenes from easily available (Z)-2-(hetero)arylidene-1-(hetero)arylbutane-1,3-diones in the presence of copper(II) oxide and iodine. This domino process involves consecutive methyl iodination/carbon–carbon double bond isomerization/6π-electrocyclization/aromatization/arene iodination sequences.

A convenient and efficient approach for the synthesis of the title imidazole and thiazole derivatives from readily available starting materials by simple solvent-switching is demonstrated.

(Oxadiazolyl)aniline derivatives (III) and (V) are obtained by a copper-catalyzed domino reaction of simple and easily available isatins and hydrazides.