Abstract
AbstractA rapid and effective approach to 4‐tosyl‐4,5‐dihydropyrazolo[1,5‐a]pyrimidines via copper‐catalyzed one‐pot cascade transformation of N‐propargylic sulfonylhydrazones with sulfonyl azides under mild conditions has been developed. This process relies on the copper‐catalyzed azide‐alkyne cycloaddition (CuAAC) and intramolecular [4+2] cycloaddition of α,β‐unsaturated hydrazone with the in situ generated ketenimine intermediate, affording the useful bicyclization products with high efficiency.magnified image
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