The Copper-Catalyzed <i>N</i>-Arylation of Indoles

Jon C. Antilla, Artis Klapars, Stephen L. Buchwald

Journal of the American Chemical Society · 2002 · 555 citations · 26 references

Concepts

Abstract

A general method for the N-arylation of indoles using catalysts derived from CuI and trans-1,2-cyclohexanediamine (1a), trans-N,N'-dimethyl-1,2-cyclohexanediamine (2a), or N,N'-dimethyl-ethylenediamine (3) is reported. N-Arylindoles can be produced in high yield from the coupling of an aryl iodide or aryl bromide with a variety of indoles.

References

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