Abstract

AbstractProtected 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.

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