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 a-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.

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

“…Medicinal chemists have employed innovative synthetic methodologies to synthesize a wide array of quinazoline compounds, incorporating diverse functional groups into the quinazoline moiety. Extensive research has been conducted to explore the potential applications of these quinazoline derivatives in the domains of biology, pesticides, and medicine [191–198] …”

“…Extensive research has been conducted to explore the potential applications of these quinazoline derivatives in the domains of biology, pesticides, and medicine. [191][192][193][194][195][196][197][198]…”