Total Synthesis of (–)‐Epothilone A

Abstract

An audacious macroaldolization is the key step in the first total synthesis of the cytotoxic epothilone A, which starts with the units 1, 2, and 3. This condensation closes the ring to form the macrolide, whose structure was determined and published (also in Angewandte Chemie) as recently as July 1996.