Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles

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

Source: Combinatorial Chemistry & High Throughput Screening, Volume 4, Number 6, September 2001 , pp. 521-524(5)

Publisher: Bentham Science Publishers

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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

Language: English

Document Type: Review article

DOI: 10.2174/1386207013330887

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