Abstract
We have developed a two steps strategy for the parallel synthesis of highly diversified quinolin-ones. In the first step we have combined and improved different synthetic methods for generating quinolin-4-ones bearing four different substitutions at specific positions using round bottomed flasks. The synthesis was assessed for a large number of substituted quinolin-4-ones. In the second step, the improved method was adapted to a parallel array synthesis using a 12 positions carrousel as demonstrated for the synthesis of 42-variable quinolin-4-ones. The first combinatorial library set 14{a-x} was obtained with a chemical purity of more than 95% without purification, the second library set 15{a-r}, which included two synthetic steps, needed combinatorial purification using an innovative parallel purifier. The proposed approach contributes to a more extensive diversification of molecular scaffolds in general and provides access to highly substituted quinolinones in particular.
Original language | English |
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Pages (from-to) | 437-448 |
Number of pages | 12 |
Journal | Molecular Diversity |
Volume | 8 |
Issue number | 4 |
DOIs | |
State | Published - 24 Nov 2004 |
Externally published | Yes |
Keywords
- 1H-quinolin-one
- scaffold decoration
ASJC Scopus subject areas
- Catalysis
- Information Systems
- Molecular Biology
- Drug Discovery
- Physical and Theoretical Chemistry
- Organic Chemistry
- Inorganic Chemistry