Mechanochemical Synthesis of Functionalized Quinolines by Iodine Mediated Oxidative Annulation.

An iodine-mediated environmentally benign synthesis of multi-substituted quinoline derivatives is developed using a solvent-free mechanochemical process. Appropriately designed and easily accessible protecting group-free aniline derivatives were used for the oxidative annulation reaction, and a series of quinoline derivatives with variable functionalities were synthesized up to 89 % isolated yield. Importantly, the activator iodine remains in the quinoline molecule and promotes further functionalizations. The present methodology is beneficial with regard to operational simplicity and mild reaction conditions.