Intramolecular Nucleophilic Addition of N‐Boc Protected α‐Amino Carbanions to Arynes: Synthesis of 1‐Aryl‐2,3,4,5‐tetrahydro‐1H‐2‐benzazepines

Abstract A two‐step protocol involving cyclization and deprotection towards the synthesis of C‐1 arylated benzazepines has been developed under transition‐metal oxidant free conditions. The coupling reaction of ‐lithiated carbanion, generated from Boc‐protected amine, with in situ generated aryne proceeds well intramolecularly. A variety of substrates were explored with corresponding products in moderate yield.