Abstract
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 benzo[e]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.
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