Brefeldin A is a natural product generated by many different microbes. Because of its interesting structure and significant antifungal, antiviral, and antitumoral activities brefeldin A has attracted remarkable attention in synthetic community since its first isolation in 1958. To date, over 30 total/formal syntheses have appeared. En route to the total syntheses many elegant synthetic methodologies and strategies were demonstrated, providing valuable knowledge to the new comers. Those syntheses published after 1997 are briefly reviewed. Some analogues are also included.

Key words: natural product, enantioselective synthesis, ring-closure reaction, antibiotics