4.8 Article

Carboxylic acid catalyzed three-component aza-Friedel-Crafts reactions in water for the synthesis of 3-substituted indoles

Journal

ORGANIC LETTERS
Volume 8, Issue 21, Pages 4939-4942

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol062031q

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The carboxylic acid catalyzed three-component aza-Friedel-Crafts reactions of aldehydes, primary amines, and indoles in water have been developed. The aza-Friedel-Crafts products could be easily transformed to various 3-substituted indoles including biologically active compounds. This system offers a novel efficient method for the synthesis of 3-substituted indoles.

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