ChemInform Abstract: Generation and Electrophile Trapping of N‐Boc‐2‐lithio‐2‐azetine: Synthesis of 2‐Substituted 2‐Azetines.

Abstract Protected methoxyazetidine undergoes α‐lithiation‐elimination to form N‐Boc‐azetine in situ, which can be further lithiated regioselectively at the sp2 center and trapped with a range of electrophiles, including allylic and propargylic halides through transmetalation to copper, affording a direct access to 2‐substituted N‐Boc azetines.