Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles

Author(s): J. Tois, R. Franzen, O. Aitio, I. Laakso, J. Huuskonen, J. Taskinen

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 4 , Issue 6 , 2001

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As part of an ongoing lead discovery project we have developed a convenient method for the modification and substitution of indole moieties at the 3-position. Selective bromination of three different 2-carboxyindoles was followed by Suzuki cross-coupling with aryl and heteroaryl boronic acids on a Merrifield resin solid-phase. After column chromatography, yields of the 3- substituted indoles ranged from 42-98 percent,

Keywords: solid phase bromination, suzuki coupling, carboxyindoles

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Article Details

Year: 2001
Page: [521 - 524]
Pages: 4
DOI: 10.2174/1386207013330887
Price: $65

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