Multicomponent formation of fused pyrroles through p-TsOH promoted N-arylation

Concise and efficient N-arylation-based domino [3+2] heterocyclization promoted by p-TsOH has been established for the synthesis of 27 examples of 3-arylamino substituted fused pyrrole derivatives in 70–90% yields. The present methodology shows attractive properties, such as mild reaction conditions, concise one-pot operation, short reaction periods of 15–30 min, and easy purification. It can avoid time-consuming and costly syntheses, tedious work-up procedures and isolation of intermediate.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide