Abstract

Phenylsulfone difluorodiazoethane (PhSO2CF2CHN2), an easy-to-prepare and bench-stable masked CF2-building block, has been developed. The synthetic utility of this reagent is demonstrated by a direct regioselective [3 + 2] cycloaddition with electron-deficient alkynes and alkenes. This protocol enables facile construction of an array of difluoromethyl-substituted pyrazoles in good to high yields under mild reaction conditions.

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