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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles

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

Volume 4, Issue 6, 2001

Page: [521 - 524] Pages: 4

DOI: 10.2174/1386207013330887

Price: $65

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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