Selective phenol alkylation: An improved preparation of efaproxiral

被引:27
作者
Anderson, Joanne E. [1 ]
Davis, Roman [1 ]
Fitzgerald, Russ N. [1 ]
Haberman, Jannine M. [1 ]
机构
[1] GlaxoSmithKline Chem Dev, Res Triangle Pk, NC 27709 USA
关键词
Bargellini reaction; 2-bromo-2-methylpropanoic acid; efaproxiral; selective alkylation;
D O I
10.1080/00397910600636527
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
收藏
页码:2129 / 2133
页数:5
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