Selective Phenol Alkylation: An Improved Preparation of Efaproxiral

Abstract

Abstract An improved, two‐step synthesis of efaproxiral, used in breast cancer therapy, is described, utilizing inexpensive commodity chemicals for starting materials. Selective amide formation and O‐alkylation in the presence of multireactive functional groups is demonstrated, thus avoiding protection/deprotection steps. Keywords: Bargellini reaction2‐bromo‐2‐methylpropanoic acidefaproxiralselective alkylation Acknowledgment The authors thank Mark S. Saulter for providing residual boron results and Hamid R. Shafiei for HPLC assistance.