Domino Synthesis of 2-Substituted Quinolines

Quinolines represent an important class of heterocycles, and the quinoline skeleton is present in various natural products, especially in alkaloids. Among them quinine is an active ingredient for the treatment of malaria [286]. Despite its relatively low efficacy and tolerability, quinine still plays an important role in the treatment of multiresistant malaria, one of the world s most devastating infectious diseases [287]. Therefore, the design of many drugs and affordable chemotherapies are based upon synthetic quinoline derivatives, such as chloroquine, mefloquine or quinacrine [288-292]. In addition, chimanine alkaloids, are also effective against parasitic diseases such as leishmaniasis and trypanosomiasis [293-295]. Besides, 

This domino methodology not only allows to access naturally occurring quinolines such as 114a and 114b (chimanine B), but also a rapid access to the antima-larial active 1,8-naphthyridine 114c, which inhibits the growth plasmodium falciparum at a lower micromolar level [297]. 

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