文摘
An operationally simple approach for the regioselective tandem synthesis of indolo[1,2-a]quinolines 4a鈥?b>v and pyrrolo[1,2-a]quinolines 5a鈥?b>k from 1-(2-bromophenyl)-1H-indole/pyrrole/imidazole 1a鈥?b>c, 2a,b by the palladium-catalyzed sequential C鈥揅 bond formation is described. The developed approach involves the palladium-catalyzed Sonogashira coupling followed by the intramolecular C鈥揅 bond formation via C鈥揌 activation, which leads to the formation of 6-endo-dig cyclized product. This synthetic methodology accommodates wide functional group variation on alkyne, which proves to be advantageous for the structural and biological activity assessments.