Synthesis and Preliminary Biological Studies of 3-Substituted Indoles Accessed by a Palladium-Catalyzed Enantioselective Alkene Difunctionalization Reaction

被引：211

作者：

Pathak, Tejas P. ^{[1
]}

Gligorich, Keith M. ^{[2
]}

Welm, Bryan E. ^{[2
]}

Sigman, Matthew S. ^{[1
,2
]}

机构：

[1] Univ Utah, Dept Chem, Salt Lake City, UT 84112 USA

[2] Huntsman Canc Inst, Dept Surg, Salt Lake City, UT 84112 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2010年 / 132卷 / 23期

基金：

美国国家卫生研究院;

关键词：

ALKYLATION;

D O I：

10.1021/ja103472a

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A unique alkene difunctionalization reaction that allows rapid construction of molecular complexity around the biologically relevant indole framework has been developed. The reaction proceeds with up to 87% yield, 99:1 er, and >20:1 dr. Evaluation of several of the compounds revealed promising anticancer activity against MCF-7 cells.

引用

页码：7870 / +

页数：3

共 18 条

[1] A journey across recent advances in catalytic and stereoselective alkylation of indoles [J].