Synthesis of Polysubstituted Fused Pyrroles by Gold-Catalyzed Cycloisomerization/1,2-Sulfonyl Migration of Yndiamides

Yndiamides (bis-N-substituted alkynes) are valuable precursors to azacycles. Here we report a cycloisomerization/1,2-sulfonyl migration of alkynyl-yndiamides form tetrahydropyrrolopyrroles, unprecedented heterocyclic scaffolds that relevant medicinal chemistry. This functional group tolerant transformation can be achieved using Au(I) catalysis proceeds at ambient temperature, and thermally promoted process. The utility the products is demonstrated by range reactions functionalize fused pyrrole core.