A remarkably faster approach towards 1,2,3-triazolyl quinolines via CuAAC in water: Their crystal structure analysis and antibacterial activities

A series of 1,2,3-triazolyl quinolines possessing substituents like -CH₂OAr (Ar = aryl) moiety on the triazolyl ring were synthesized via a multi-step sequence consisting of copper-catalyzed azide-alkyne cycloaddition (CuAAC) of 3-(azidomethyl)-quinoline derivative with terminal alkynes as a key step. This step was found to be remarkably faster in pure water and completed within 10-45 min. The robustness of this step was demonstrated by synthesizing a large number of compounds some of which showed promising antibacterial activities when tested in vitro. The crystal structure analysis of a representative compound along with hydrogen bonding patterns and molecular arrangement present within the molecule is described.