Synthesis of Diverse Allylic Sulfone Derivatives via Sequential Hydroalkoxylation of 1,3-Enynes.

A first metal-free protocol for the synthesis of allylic sulfones featuring aldehyde functionality at the δ-position has been reported. The formation of structurally complex δ,δ-dimethoxy allylic sulfones is enabled by the direct nucleophilic attack of methoxide onto the sulfone-containing 1,3-enynes. The present approach allows facile installation of acetal groups within the allylic sulfone scaffold, providing versatile platforms for further functionalization and drug development.