I-TBHP-catalyzed azomethine imine generation and subsequent regioselective 1,3-dipolar cycloaddition (DC) with aromatic N-heterocycles was developed to afford various 4,3-fused 1,2,4-triazoles in excellent yields. The method is operationally simple and highly efficient with broad functional group tolerance.
An unprecedented and highly efficient multicomponent domino reaction for construction of various 4,3-fused 1,2,4-triazoles from readily available starting materials such as aldehydes, ptoluenesulfonhydrazide and aromatic N-heterocycles catalyzed by KI/TBHP system has been developed. The method is transition metal free, operationally simple, eco-friendly and inexpensive with broad functional group tolerance. This unique methodology was further expanded toward a new concept of multicomponent diversity oriented synthesis (DOS) to generate various 4,3-fused 1,2,4-triazoles using a combination of multiple N-heterocycles and aldehydes, all in one-pot, to give the corresponding products.
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