Experimental study reveals efficient acetic acid-catalyzed cyclization yielding trans-dihydropyrazoles, suggesting a practical synthetic pathway for multi-substituted heterocycles.
Acetic acid-catalyzed (3 + 2) cyclization reaction of substituted 2-aroyl-3-aryl-1,1-dicyanocyclopropanes with arylhydrazines was investigated for the efficient synthesis of 4-dicyanomethyl-1,3,5-triaryl-4,5-dihydropyrazoles in good yields, in which 4,5-double substituents are predominantly trans selective. This approach included the consecutive condensation, ring opening, and double nucleophilic cyclization reaction.
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Xue et al. (2023) studied this question.
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