Diversity-oriented synthesis of tamoxifen-type tetrasubstituted olefins

被引：194

作者：

Itami, K ^{[1
]}

Kamei, T ^{[1
]}

Yoshida, J ^{[1
]}

机构：

[1] Kyoto Univ, Grad Sch Engn, Dept Synthet Chem & Biol Chem, Nishikyo Ku, Kyoto 6158510, Japan

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2003年 / 125卷 / 48期

关键词：

D O I：

10.1021/ja037566i

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A general synthetic scheme for tamoxifen-type tetrasubstituted olefins based on the novel Cu-catalyzed carbomagnesation across alkynyl(2-pyridyl)silane has been developed. A wide array of electronically and structurally diverse tetrasubstituted olefins can be prepared in a regiocontrolled, stereocontrolled, and diversity-oriented manner. Noteworthy features are that (i) the three aryl groups, which are believed to be important (essential) for anti-estrogenic activity, can be varied at will because they all stem from readily available aryl iodides, and (ii) any stereo- and regioisomers can, in principle, be prepared by simply changing the applying order of aryl iodides into the sequence. Copyright © 2003 American Chemical Society.

引用

页码：14670 / 14671

页数：2

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