Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles

J.      Tois; R.      Franzen; O.      Aitio; I.      Laakso; J.      Huuskonen; J.      Taskinen

doi:10.2174/1386207013330887

Abstract

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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Combinatorial Chemistry & High Throughput Screening

Title: Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles

Volume: 4 Issue: 6

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

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Keywords: solid phase bromination, suzuki coupling, carboxyindoles

Abstract: 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,

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Tois J., Franzen R., Aitio O., Laakso I., Huuskonen J. and Taskinen J., Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles, Combinatorial Chemistry & High Throughput Screening 2001; 4 (6) . https://dx.doi.org/10.2174/1386207013330887