Zhang Bo, Studer Armido
Westfälische Wilhems-University, Institute of Organic Chemistry, Corrensstraße 40, 48149, Münster, Germany.
Org Biomol Chem. 2014 Dec 28;12(48):9895-8. doi: 10.1039/c4ob02145b.
A simple and efficient approach to biologically important 1-trifluoromethylated isoquinolines starting with readily prepared β-aryl-α-isocyano-acrylates and the commercially available Togni reagent as the CF3 radical precursor is described. These transformations occur in the absence of any transition metals and the title compounds are obtained in moderate to excellent yields. This protocol comprises a trifluoromethylation with concomitant isoquinoline framework construction.
描述了一种从易于制备的β-芳基-α-异氰基丙烯酸酯和市售的Togni试剂作为CF3自由基前体出发，制备具有生物学重要性的1-三氟甲基异喹啉的简单有效方法。这些转化在没有任何过渡金属的情况下发生，并且目标化合物以中等至优异的产率获得。该方案包括伴随异喹啉骨架构建的三氟甲基化反应。
