Gold Catalyzed 7-endo-dig Hydroaminations Yielding 1,4-Diazepineones

Strategies to access the 1,4-diazepindiones heterocyclic core of the TAN-1057 family of natural products revealed a successful gold-catalyzed hydroamination of yneamide tethered amines. The precursor amino-yneamides are derived from easily accessible 1,2-diamines and alkynoic acids and are efficiently cyclized to the corresponding diazepineones.