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Synlett 1994; 1994(1): 93-94
DOI: 10.1055/s-1994-22752
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Synthesis of 6- and 7-Arylindoles via Palladium-Catalyzed Cross-Coupling of 6- and 7-Bromoindole with Arylboronic Acids

George M. Carrera, Jr.* , George S. Sheppard
  • *Abbott Laboratories, Immunoscience Research, Department 47J, Abbott Park, IL 60064 USA
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Publication Date:
22 March 2002 (online)

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Couplings of 6- and 7-bromoindole with various arylboronic acids were effected via the Suzuki reaction. This method provided good yields and was found to be suitable for scale-up to 10-20 grams of the desired arylindole products. The primary advantage of this cross-coupling method is that indole functionalization or nitrogen protection is unnecessary. Also, during these investigations a known synthesis of 6-bromoindole was improved, and the revised procedure is amenable to large-scale preparation.

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