- Automated multistep continuous flow synthesis of 2-(1H-indol-3-yl)thiazole derivatives
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The multistep continuous flow assembly of 2-(1H-indol-3-yl)thiazoles using a Syrris AFRICA synthesis station is reported. Sequential Hantzsch thiazole synthesis, deketalization, and Fischer indole synthesis provides rapid and efficient access to highly functionalized, pharmacologically significant 2-(1H-indol-3-yl)thiazoles. These complex drug-like small molecules are generated in reaction times of less than 15 minutes and in high yields (38-82% over three chemical steps without isolation of intermediates). Georg Thieme Verlag Stuttgart · New York.
- Pagano, Nicholas,Heil, Marintha L.,Cosford, Nicholas D. P.
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experimental part
p. 2537 - 2546
(2012/09/05)
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- EXTRUSION REACTIONS-VII. FORMATION OF 2,5-DIARYL-1,4-DITHIINS AND 2-ACETONYL THIAZOLES
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ω-(2,6-Dimethyl-4-pyrimidinylthio-(4), 2-methyl-4-quinazolinylthio-(9), and 4-oxo-2-quinazolinylthio)-(10) acetophenones with hydrochloric or perchloric acid provide 2,5-diaryl-1,4-dithiins (7) whereas ω-(6-methyl-4-pyrimidinylthio)acetophenones (11) with aq HCl/HClO4 or POCl3 followed by hydrolysis provide 1-(4-aryl-2-thiazolyl)-2-propanones (12).Likewise, 2-(6-methyl-4-pyrimidinylthio)cyclohexanone (13) give the thiazole derivative (14).
- Singh, Harjit,Aggarwal, Sunil K.,Malhotra, Nageshwar
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p. 4941 - 4946
(2007/10/02)
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