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Selective Phenol Alkylation: An Improved Preparation of Efaproxiral |
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| Authors: | Joanne E Anderson Russ N Fitzgerald Jannine M Haberman |
| Institution: | GlaxoSmithKline Chemical Development , Research Triangle Park, North Carolina, USA |
| 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 reaction 2‐bromo‐2‐methylpropanoic acid efaproxiral selective alkylation |