A facile synthesis of 3-trifluoromethyl-1,2,4-oxadiazoles from cyanamides

被引:19
作者
Goldberg, Kristin [1 ]
Clarke, David S. [1 ]
Scott, James S. [1 ]
机构
[1] AstraZeneca, Cardiovasc & Gastrointestinal Innovat Med Unit, Macclesfield SK10 4TG, Cheshire, England
关键词
3-Trifluoromethyl-1,2,4-oxadiazoles; Cyanamides; N-Boc-hydroxylamine; 1,2,4-Oxadiazoles; NITRILE OXIDES; CYCLOADDITION; OPTIMIZATION;
D O I
10.1016/j.tetlet.2014.06.019
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A safe and facile method for the formation of 3-trifluoromethyl-5-amino-1,2,4-oxadiazoles, via a reversed addition of hydroxylamine to cyanamides, is reported. This two-pot procedure is suitable to scale-up and avoids the hazards associated with trifluoromethyl amidoxime synthesis. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4433 / 4436
页数:4
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