β‐Lactam‐Synthon‐Interceded, Facile, One‐Pot, Diastereoselective Synthesis of Functionalized Tetra/Octahydroisoquinolone Derivatives

Abstract

Abstract The convenient and facile synthesis of tetra/octahydroisoquinolones has been developed and validated by using inter/intramolecular amidolysis of racemic N ‐aryl‐β‐lactams followed by intramolecular iodocyclization protocols. Thesingle‐pot synthetic version of the desired conversion was successfully developed. The single‐pot synthesis of tetrahydro‐4 H ‐isoquinoline‐1,3‐diones invariably resulted in aromatic electrophilic iodination rather than the desired iodocyclization in cases where N ‐phenyl‐2‐azetidinones were employed as the synthetic precursors.