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Bischler Indole Synthesis under Microwave Irradiation: A Solvent-Free Synthesis of 2-Arylindoles
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1  Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain

Abstract: The solid-state reaction between anilines and phenacyl bromides in the presence of an equimolecular amount of sodium bicarbonate gives phenacylanilines. Microwave irradiation of mixtures of these compounds with anilinium bromides at 560 W for 45-60 s provides a general, solvent-free method for the synthesis of 2-arylindoles in 50-56% overall yields. A one-pot variation of the method, involving irradiation of 2:1 mixtures of anilines and phenacyl bromides, allowed a simplified experimental procedure and led to improved yields (52-75%).

 
 
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