Annulative Coupling of β‑Ketosulfoxonium Ylides, β‑Ketothioamides, and Aldehydes: Access to Highly Functionalized Dihydrothiophenes

A one-pot
strategy has been developed for the efficient synthesis
of highly functionalized dihydrothiophenes using β-ketosulfoxonium
ylides, β-ketothioamides, and aldehydes. This cascade process
involves C(sp3)–H insertion, aldol condensation,
and intramolecular 1,4-conjugate addition, forming C–S and
C–C bonds efficiently. The method offers good to high yields,
a broad substrate scope, structural diversity, and scalability. Additionally,
its synthetic utility is demonstrated through further transformation
into a thiophene derivative, highlighting its applicability in the
construction of complex molecules.