Rapid Access to Stereochemically Defined Heterocyclic Scaffolds

Significance

This work describes the rhodium(I)-mediated ring opening of hetaryne-furan Diels-­Alder adducts, the unexplored class of compounds in the context of transition-metal catalysis. Various types of heterocyclic substrates 2-5 have been screened. The resulting derivatives are interesting as being analogous to bioactive products (2-aminotetralins), and thus can be used in diversity-oriented synthesis of potential drug ­candidates.