Construction of Fused Heterocyclic Architectures by Formal [4+1]/[3+2] Cycloaddition Cascade of Sulfur Ylides and Nitroolefins

Under control: A formal [4+1]/[3+2] cycloaddition cascade of sulfur ylides and alkene-tethered nitroolefins has been developed, and provides an efficient synthesis of fused polycyclic heterocyclic compounds in good to excellent overall yields with excellent diastereocontrol (see scheme). A catalytic asymmetric variant of this reaction has also been disclosed.