Microwave‐assisted Three‐component Reactions for Regioselective Synthesis of Functionalized Benzo[e]indoles

Microwave‐assisted three‐component reactions of arylglyoxals with cyclic 1,3‐dicarbonyl compounds and naphthalen‐2‐amine have been established, by which a series of new functionalized benzoe ]indoles with good yields were synthesized. The reaction was easily conducted in HOAc, enabling domino cyclization to construct three new σ‐bonds in a one‐pot operation. Flexible structural modification and broad functional group compatibility as well as mild reaction conditions make this strategy a useful and attractive process of library generation for drug discovery.