A General One-pot Two-step Protocol Accessing a Range of Novel Polycyclic Heterocycles with High Skeletal Diversity

摘要

An Ugi one-pot three-component 4-center reaction was coupled with a subsequent acid mediated cyclodehydration step to furnish a multitude of unique scaffolds having in common an embedded or attached benzimidazole and often a ring system formed through lactamization. Using combinations of tethered Ugi inputs typically via tethered acid-ketone inputs and supporting reagents containing masked internal nucleophiles, such scaffolds were produced in good to excellent yields in an operationally friendly manner.