An Eco-Friendly Synthetic Approach through C(sp3)-H Functionalization of the Viral Fusion “Spike Protein” Inhibitors

Abstract

The use of organic chemistry to synthesize bio-relevant molecules has been a prime interest of the drug discovery sentients. Recently, our group found 2-styryl substituted quinoline as an anticancer and viral fusion inhibitor through the binding of the gp-41 spike protein. So, we through to synthesize various molecules with an eco-friendly approach. However, various approaches have been reported with the metal, additive, base, and acids to synthesize highly important 2-styrylquinoline from the 2-alkyl quinoline. Still, none of the approaches was reported with the restricted 4-hydroxyquinoline substrate because of their dual nucleophilic nature. The selectivity raises an important issue in this concern substrate. The present protocol overcomes the dual nucleophilic character of the hydroxyl-linked substrate through an optimized eco-friendly sp3 C-H activation approach. The designed protocol for synthesizing gp-41 inhibitors as viral entry inhibitors claimed as metal, acid, and base along with the solvent-free protocol.