Assembly of 4-aminoquinolines via palladium catalysis:: A mild and convenient alternative to SNAr methodology

被引：62

作者：

Margolis, Brandon J. ^{[1
]}

Long, Kimberly A. ^{[1
]}

Laird, Dana L. T. ^{[1
]}

Ruble, J. Craig ^{[1
]}

Pulley, Shon R. ^{[1
]}

机构：

[1] Eli Lilly & Co, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2007年 / 72卷 / 06期

关键词：

D O I：

10.1021/jo062168u

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

4-Aminoquinolines, classically prepared via SNAr chemistry from an amine and 4-haloquinoline, are important scaffolds in medicinal chemistry. Interest in these compounds prompted us to explore palladium catalysis as an alternative to the existing methods for their preparation. Initial results followed by an iterative screening paradigm confirmed Pd(OAc)(2)/ DPEphos/K3PO4 as a mild and convenient alternative for the formation of the C-N bond in 4-aminoquinolines. A description of the screen and the scope of this methodology are discussed herein.

引用

页码：2232 / 2235

页数：4

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