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.
引用
收藏
页码：6901 / 6903
页数：3
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