Synthetic study demonstrates efficient cascade synthesis of 2-aminothiochromones via thiocarbonyldiimidazole under mild conditions, suggesting a concise pathway to diverse sulfur heterocycles.
A highly efficient cascade synthesis of various substituted 2-aminothiochromones was developed. The commercially available thiocarbonyldiimidazole (TCDI) acted as a key precursor in the construction of a sulfur-containing scaffold from 2-fluorophenyl ketone. Subsequent conjugated addition–elimination resulted in the corresponding 2-aminothiochromones under mild conditions. This simple protocol tolerates a broad range of functional groups and provides concise access to various 2-aminothiochromones in good to excellent yields (up to 94%).
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Zhang et al. (2026) studied this question.
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