Abstract: A convergent aromatic annulation strategy based on the thermal combination of heterosubstituted acetylenes and cyclobutenones has been applied in an efficient total synthesis of the antitumor antibiotic mycophenolic acid. The key annulation components 3 and 4 are rapidly assembled by straightforward routes and then heated in benzene at 120 OC for 14 h. This annulation reaction generates the pentasubstituted aromatic ...