Abstract

A base-promoted [3 + 2] cycloaddition of 2-chloro-2-trifluoromethylstyrenes with tosylhydrazones has been established. This one-pot reaction provides a practical and efficient method for the selective synthesis of 4-trifluoromethylpyrazoles through the domino sequence of dehydrochlorination, detosylation, cyclization and 1,3-hydrogen atom transfer process. The tandem reaction features mild conditions and good functional group tolerance from easily prepared CF3-building blocks.

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