Pd-Catalyzed Nucleophilic Fluorination of Aryl Bromides

被引：121

作者：

Lee, Hong Geun ^{[1
]}

Milner, Phillip J. ^{[1
]}

Buchwald, Stephen L. ^{[1
]}

机构：

[1] MIT, Dept Chem, Cambridge, MA 02139 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2014年 / 136卷 / 10期

基金：

美国国家卫生研究院; 美国国家科学基金会;

关键词：

COPPER-MEDIATED FLUORINATION; LATE-STAGE FLUORINATION; MEDICINAL CHEMISTRY; FLUORIDE; CONVERSION; PALLADIUM; CHLORIDES; F-18; PET;

D O I：

10.1021/ja5009739

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

On the basis of mechanism-driven reaction design, a Pd-catalyzed nucleophilic fluorination of aryl bromides and iodides has been developed. The method exhibits a broad substrate scope, especially with respect to nitrogen-containing heteroaryl bromides, and proceeds with minimal formation of the corresponding reduction products. A facilitated ligand modification process was shown to be critical to the success of the reaction.

引用

页码：3792 / 3795

页数：4

共 30 条

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