Total synthesis of 26-hydroxy-epothilone B and related analogs via a macrolactonization based strategy

Article abstract of DOI:10.1016/S0040-4020(98)00352-4

The chemical synthesis of a series of 26-substituted epothilones B is described. Fully protected 26-hydroxydesoxy-epothilone B (7), prepared via the macrolactonization strategy, served as a common precursor to the designed epothilones described. The synthesized compounds were members of a large epothilone library whose biological screening led to the identification of a number of highly potent antitumor agents.