Pyrrolidines and sulfocoumarins are ubiquitous structural motifs present in numerous natural products, pharmaceuticals and biologically active molecules. For instance, Kainic acid 1 is a typical pyrrolidine containing natural product that can be found in marine algae, which exhibits interesting anthelmintic activity. Product b 2 can be used as noncompetitive antagonists of the muscular nicotine receptor and AChE inhibitor. Product c 3 exhibits anticancer activity. Product d could act as a human carbonic anhydrases inhibitor. Considering the significance of both pyrrolidines and sulfocoumarins, the development of efficient method for the synthesis of pyrrolidine fused sulfocoumarins will be highly important for drugs discovery.