SYNTHESES OF ZINDOXIFENE AND ANALOGS BY TITANIUM-INDUCED OXO-AMIDE COUPLING

被引：28

作者：

FURSTNER, A

JUMBAM, DN

SEIDEL, G

机构：

[1] Max-Planck-Institut Für Kohlenforschung, Mülheim, D-45470, Kaiser‐Wilhelm‐Platz 1, Ruhr

来源：

CHEMISCHE BERICHTE | 1994年 / 127卷 / 06期

关键词：

INDOLES; 2-ARYL; TITANIUM GRAPHITE; ZINDOXIFENE; TUMOR-GROWTH INHIBITORS; ALKYLIDENATION; INTRAMOLECULAR;

D O I：

10.1002/cber.19941270624

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Highly reactive titanium on graphite is used to reductively cyclize electron-rich acylamino carbonyl compounds 7, 8, 12, 14, and 16 to the corresponding indole derivatives 9, 10, 13, 15, and 17. Compound 9b is a known precursor of the mammary tumor-inhibiting compound zindoxifene (2). The other products are new analogues of this anticancer drug, exhibiting the substitution pattern previously recognized to be essential for high pharmacological activity.

引用

页码：1125 / 1130

页数：6

共 30 条

[1] ETHER CLEAVAGE BY ACTIVATED METALS .1. CLEAVAGE OF TETRAHYDROFURAN BY TRANSITION-METAL ACTIVATED MAGNESIUM [J].