Aza- ortho -Quinone Methide Promoted Strain-Release-Driven Conversion of Azabicyclo[1.1.0]butanes into Functionalized Azetidines

A strategy for activating azabicyclo[1.1.0]butane (ABB) with in situ generated aza- ortho -quinone methide, promoted by HFIP, is reported. This unified activation, vis-à-vis strain-release-driven N/C3-functionalization, features a new means to prepare functionalized azetidines from ABB. Additionally, the newly installed motif on azetidine nitrogen could be forged into an indoline via Pd-catalyzed hydroamination, leveraging access to medicinally relevant scaffolds.