The difunctionalization reactions of easily available and inexpensive alkynes have emerged as a reliable, powerful, and step-economical approach for the construction of highly substituted complex alkenes in a one-pot manner, without the need for isolation of intermediates. A wide variety of transformations based on this concept have been successfully achieved for the preparation of synthetically and biologically important β-halovinyl sulfone scaffolds. In this Review, we summarize the recent advances and developments in this field and present a comprehensive overview of halosulfonylation of alkyne substrates with emphasis on the mechanistic features of the reactions.
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