氰基乙酰胺（IV）：一种通用的一锅法合成 2-喹啉-3-甲酰胺的方法。
Cyanoacetamides (IV): versatile one-pot route to 2-quinoline-3-carboxamides.
机构信息
University of Pittsburgh , Drug Discovery Institute, Biomedical Science Tower 3, 3501 Fifth Avenue, Pittsburgh, Pennsylvania 15261, United States.
出版信息
ACS Comb Sci. 2012 May 14;14(5):316-22. doi: 10.1021/co3000133. Epub 2012 Apr 18.
Abstract
Cyanoacetic acid derivatives are the starting materials for a plethora of multicomponent reaction (MCR) scaffolds. Herein, we describe scope of a valuable general protocol for the synthesis of arrays of 2-aminoquinoline-3-carboxamides from cyanoacetamides and 2-aminobenzaldehydes or heterocyclic derivatives via a Friedländer reaction variation. In many cases, the reactions involve a very convenient work up by simple precipitation and filtration. More than 40 new products are described. We foresee our protocol and the resulting derivatives becoming very valuable to greatly expanding the scaffold space of cyanoacetamide derivatives.
摘要
氰基乙酸衍生物是多种多组分反应（MCR）支架的起始原料。在此，我们描述了一种有价值的通用方法的范围，该方法可通过 Friedländer 反应变化从氰乙酰胺和 2-氨基苯甲醛或杂环衍生物合成 2-氨基喹啉-3-甲酰胺的阵列。在许多情况下，反应通过简单的沉淀和过滤非常方便地进行后处理。描述了 40 多种新产品。我们预计我们的方案和得到的衍生物将非常有价值，可大大扩展氰乙酰胺衍生物的支架空间。
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