Divergent Synthesis of 2‐Quinolinyl‐Substituted Thiophenes Via Acid‐Promoted Three‐Component Cyclization

Bisheteroaryls and its derivatives, as a privileged motifs, are commonly found in natural products, pharmaceuticals, ligands, and other bioactive molecules. Herein, a novel and efficient method for the divergent synthesis of functional 2‐quinolinyl‐bearing thiophenes via acid‐mediated three‐component cyclization of 2‐methylquinolines, S powder, and chromone‐3‐carbaldehydes or enals is reported. This approach stands out due to its metal‐free conditions, readily available starting materials, broad substrate scopes, simple operation, and the efficient formation of multibonds in one‐pot. The Gram scale reaction and useful derivatizations are performed to showcase the potential synthetic utility of this strategy. This acid‐promoted cyclic strategy provides a straightforward pathway toward diversely valuable thiophenes, which possibly exhibit good applications in medicinal chemistry and materials science.