Wang Kan, Nguyen Katrina, Huang Yijun, Dömling Alexander
University of Pittsburgh, Drug Discovery Institute, Pittsburgh 15261, Pennsylvania, USA.
J Comb Chem. 2009 Sep-Oct;11(5):920-7. doi: 10.1021/cc9000778.
Cyanoacetic acid derivatives are the starting materials for a plethora of multicomponent reaction (MCR) scaffolds. However the diversity of these scaffolds is hampered by the low variability of the cyanoacetic acid derivatives in the past. Here we describe valuable protocols for the parallel synthesis of arrays of cyanoacetamides on a multigram scale and involving very convenient work up by simple filtration and washing. Fifty-two products are described, and several applications are indicated. We foresee our protocol and the resulting derivatives to become very valuable to greatly expanding the large MCR scaffold space of cyanoacetic acid derivatives.
氰基乙酸衍生物是众多多组分反应(MCR)支架的起始原料。然而,过去氰基乙酸衍生物的低变异性阻碍了这些支架的多样性。在此,我们描述了在多克规模上平行合成氰基乙酰胺阵列的有价值的方法,该方法通过简单过滤和洗涤即可轻松完成后处理。文中描述了52种产物,并指出了几种应用。我们预计我们的方法及所得衍生物对于极大地扩展氰基乙酸衍生物的大型MCR支架空间将变得非常有价值。