A chemoselective aniline-chloropyrimidine coupling in a competing electrophilic environment

被引：27
作者：
Choudhury, Anusuya [1 ]
Chen, Hongfeng [1 ]
Nilsen, Christopher N. [1 ]
Sorgi, Kirk L. [1 ]
机构：
[1] LLC, Johnson & Johnson Pharmaceut Res & Dev, Chem Dev, Raritan, NJ 08869 USA
来源：
TETRAHEDRON LETTERS | 2008年 / 49卷 / 01期
关键词：
Acid catalyzed coupling; Chloropyrimidine; Diaminopyrimidines;
D O I：
10.1016/j.tetlet.2007.11.009
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A highly chemoselective substitution on 4-amino-6-chloropyrimidine ring system having a competing aldehyde functionality has been realized with anilines which produces 4, 6-diaminopyrimidine-5-carbaldehyde in high yield. The reaction may involve the intermediacy of imines. A variety of aromatic amines participate in this reaction successfully to generate diaminopyrimidine aldehydes in moderate to high yield. (C) 2007 Elsevier Ltd. All rights reserved.
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收藏
页码：102 / 105
页数：4
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