Automated multistep continuous flow synthesis of 2-(1H-indol-3-yl)thiazole derivatives

摘要

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).