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ABSTRACT: An easy three-step pathway for the synthesis of arylacetaldehydes from the corresponding carboxylic acids in very high yields is described. Their use as precursors of 5-substituted 2-aminothiophenes is illustrated via a microwave-assisted Gewald reaction. This method allows obtaining the expected compounds in a shorter time and with better yields and purities than the classical procedures.
Synthesis 01/2011; 2011:2935. · 2.47 Impact Factor
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ABSTRACT: 2-Thiazolylimino-1,3-thiazolidin-4-one derivatives have already been described as compounds with anti-tumor, anti-inflammatory or anti-bacterial activities. Their structural common moiety with the glitazone class of compounds, which are known to present activities against colon cancer cell lines, led us to consider that other thiazolidinone derivatives could also present biological properties against HT29 cancer cells.
For many years, our group has been interested in the synthesis of heterocycles like thiophenes, selenophenes and thiazoles. Starting from 2-aminothiophenes/selenophenes, we synthesized new series of heteroarylimino-1,3-thiazolidin-4-ones, with various substitutions on the thiazolidinone ring, which were assayed for viability on HT29 cells derived from human colon adenocarcinoma with interesting results.
RICT XLVIII, Lyon; 01/2011
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ABSTRACT: The preparation of N-substituted 2-arylimino-1,3-thiazolidin-4-ones from 5-substituted-3-aminothiophenes using an easy three-step procedure is described.
Synthesis 01/2010; 2010:3319. · 2.47 Impact Factor
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ABSTRACT: 2-Thiazolylimino-1,3-thiazolidin-4-one derivatives have already been described as compounds with anti-tumor, anti-inflammatory or anti-bacterial activities.
In continuation of syntheses already developed in our laboratory, we decided to synthesize new thiazolidinone scaffolds starting from 3-aminothiophene-2-carboxylates.
Those thiophenes are prepared by a well-described procedure from β-chloroacrylonitriles obtained from the enolisable ketones via a Vilsmeier-Haack-Arnold reaction.
The targeted thiazolidinones were obtained through the 3-aminothiophene intermediate using two different ways depending on the substitution of the nitrogen from the thiazolidinone ring.
Biological tests on those compounds are ongoing in our lab.
BOSS XII, Namur; 01/2010
