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LZX1024

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Abstract: In the past decade alkynes have become attractive starting materials for the synthesis of a variety of indole derivatives. This review summarizes the development of diverse homogeneous catalytic methods for the synthesis of indoles from alkynes and different N nucleophiles such as arylhydrazines, aniline derivatives, aryl isonitriles and nitroarenes.
1 Introduction
2 Metal-Catalyzed Hydroamination of Alkynes with Arylhydrazines
3 Indoles from Aniline Derivatives
3.1 Annulation of o-Haloanilines with Alkynes
3.2 Cyclization of o-Alkynylaniline Derivatives
3.3 Reaction of Anilines with Propargyl Alcohol Derivatives
4 Indoles from Isocyanides
5 Cycloaddition of Nitro- and Nitrosoarenes with Alkynes
6 Conclusion
Keywords: alkynes; anilines; hydrazines; indoles; isonitriles; nitroarenes

The indole ring system is the most widely distributed heterocycle found in nature. Since indole was first isolated by treatment of indigo dye with oleum, the name indole is a combination of the words indigo and oleum. Among the numerous structurally diverse derivatives many indoles show significant biological activity such as tryptamine, tryptophan, and serotonin. Hence, it is not surprising that this structural motif is also an important component in many of todayBs pharmaceuticals (Scheme 1).

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