Selective synthesis of 2-substituted pyridine N-oxides via directed ortho-metallation using Grignard reagents

被引：28

作者：

Andersson, Hans ^{[2
]}

Gustafsson, Magnus ^{[1
]}

Olsson, Roger ^{[1
]}

Almqvist, Fredrik ^{[2
]}

机构：

[1] ACADIA Pharmaceut AB, S-20512 Malmo, Sweden

[2] Umea Univ, Dept Chem, SE-90187 Umea, Sweden

来源：

TETRAHEDRON LETTERS | 2008年 / 49卷 / 48期

关键词：

D O I：

10.1016/j.tetlet.2008.09.104

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Addition of i-PrMgCl to pyridine N-oxides in THF at -78 degrees C generates selectively an ortho-metallated species, which can he trapped with various electrophiles to generate 2-substituted pyridine N-oxides. Furthermore, by applying a double metal-catalyzed cross-coupling, direct arylation of the pyridine N-oxides is achieved. (c) 2008 Elsevier Ltd. All rights reserved.

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页码：6901 / 6903

页数：3

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