Syntheses of enantiomerically pure (R)- and (S)-bicalutamide

被引：26

作者：

James, KD ^{[1
]}

Ekwuribe, NN ^{[1
]}

机构：

[1] Nobex Corp, Dept Innovat, Durham, NC 27713 USA

来源：

TETRAHEDRON | 2002年 / 58卷 / 29期

关键词：

antiandrogen; enantiomeric purity; bicalutamide; Casodex (R); citramalic acid;

D O I：

10.1016/S0040-4020(02)00560-4

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The racemic antiandrogen bicalutamide is the leading antiandrogen used for the treatment of prostate cancer. The (R)-isomer possesses virtually all of the activity, but both isomers are metabolized by the liver. A convenient synthetic route to the active enantiomer would be an attractive option for patients who are hepatically impaired. We now demonstrate a rather short synthesis of (R)-bicalutamide, starting with a naturally occurring, chiral precursor. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：5905 / 5908

页数：4

共 22 条

[1] A PRACTICAL ALTERNATIVE TO THE HUNSDIECKER REACTION [J].