Department of Chemistry, Université de Montréal, P.O. Box 6128, Station Downtown, Montréal, Quebec, Canada H3C 3J7.
Org Lett. 2010 Feb 5;12(3):516-9. doi: 10.1021/ol902710f.
The synthesis of 2-substituted pyrazolo[1,5-a]pyridines from N-iminopyridinium ylides is described. These medicinally interesting compounds are formed through a cascade process involving a palladium-catalyzed direct alkenylation reaction followed by silver-mediated cyclization. The reaction can be performed with a wide range of electron-poor and electron-rich alkenyl iodides in good yields. This work represents perhaps the most direct route for the preparation of these compounds.
本文描述了从 N-亚氨基吡啶翁叶立德合成 2-取代的吡唑并[1,5-a]吡啶。这些具有医学意义的化合物是通过级联过程形成的,其中包括钯催化的直接烯基化反应和银介导的环化反应。该反应可以使用广泛的缺电子和富电子烯基碘化物,以良好的收率进行。这项工作代表了制备这些化合物的最直接途径。