posted on 2024-02-27, 19:24authored byQiang Yan, Zhe Zhuang, Rong Fan, Jingwen Wang, Tuanli Yao, Jiajing Tan
N-Aryl (iso)quinolones are of increasing
interest
in material and medicinal chemistry, although general routes for their
provision remain underexplored, especially when compared with its N-alkyl counterparts. Herein, we report a modular and transition-metal-free,
aryne-induced three-component coupling protocol that allows the facile
synthesis of structurally diverse N-aryl (iso)quinolones
from readily accessible halo-(iso)quinolines in the presence of water.
Preliminary results highlight the applicability of our method through
scale-up synthesis, downstream derivatization, and flexible synthesis
involving other types of aryne precursors.