Solid-phase bromination and Suzuki coupling of 2-carboxyindoles

Authors
Tois, J Franzen, R Aitio, O Laakso, I Huuskonen, J Taskinen, J
Citation
J. Tois et al., Solid-phase bromination and Suzuki coupling of 2-carboxyindoles, COMB CHEM H, 4(6), 2001, pp. 521-524
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
ISSN journal
13862073 → ACNP
Volume
4
Issue
6
Year of publication
2001
Pages
521 - 524
Database
ISI
SICI code
1386-2073(200109)4:6<521:SBASCO>2.0.ZU;2-W
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-p osition. Selective bromination of three different 2-carboxyindoles was foll owed by Suzuki cross-coupling with aryl and heteroaryl boronic acids on a M errifield resin solid-phase. After column chromatography, yields of the 3- substituted indoles ranged from 42-98%.