Solid-phase bromination and Suzuki coupling of 2-carboxyindoles
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Details
| Original language | English |
|---|---|
| Pages (from-to) | 521-524 |
| Number of pages | 4 |
| Journal | Combinatorial Chemistry and High Throughput Screening |
| Volume | 4 |
| Issue number | 6 |
| DOIs | |
| Publication status | Published - 2001 |
| Externally published | Yes |
| Publication type | A1 Journal article-refereed |
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%.