Iodide-Catalyzed Intermolecular Formal (3 + 3) Cycloaddition of Bicyclo1.1.0butanes and Amides: Modular Access to Heteroatom-Enriched Bicyclo3.1.1heptane Scaffolds

Key Points

• The research investigates a new iodide-catalyzed method for creating heterobicyclo[3.1.1]heptane structures.
• Iodide-catalyzed formal (3 + 3) cycloaddition of bicyclo[1.1.0]butanes and amides
• Metal-free approach with wide functional group tolerance
• Focus on late-stage diversification of molecules.
• Successful synthesis of 2-oxa-4-azabicyclo[3.1.1]hept-3-enes
• The method allows for modular access to sp3-rich structures
• Demonstrated practical application in drug discovery for creating pyridine bioisosteres.