55788-90-4Relevant academic research and scientific papers
Metal-Free Cascade Annulation Approach for Modular Assembly of Alkynyl/Benzoyl Functionalized Quinolines
Tang, Qiang,Yuan, Meng,Duan, Jiahui,Xu, Keke,Li, Ruxue,Xie, Mengqing,Kong, Shuwen,He, Xinwei,Shang, Yongjia
supporting information, (2022/01/19)
A concise and efficient synthetic method for alkynyl quinolines through TfOH-promoted cascade 1,4-conjugate addition/intramolecular annulation/aromatization process is established. By virtue of reactive aza-o-AQM (in situ generated from modular propargylamine), this reaction proceeds smoothly to afford a variety of alkynyl quinolines in good to excellent yields. This transition-metal-free process features halogen groups tolerance, such as the ?Cl, ?Br, and ?I groups; thus, this protocol circumvents the inherent shortcomings of the existing Sonogashira coupling of halogenated quinolines.
