Department of Chemistry, University of Oxford, Chemistry Research Laboratory, Mansfield Road, Oxford OX1 3TA, United Kingdom.
Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11605-8. doi: 10.1073/pnas.1206532109. Epub 2012 Jul 2.
The utilization of sequential palladium-catalyzed α-arylation and cyclization reactions provides a general approach to an array of isoquinolines and their corresponding N-oxides. This methodology allows the convergent combination of readily available precursors in a regioselective manner and in excellent overall yields. This powerful route to polysubstituted isoquinolines, which is not limited to electron rich moieties, also allows rapid access to analogues of biologically active compounds.
通过钯催化的连续α-芳基化和环化反应的利用,为一系列异喹啉及其相应的 N-氧化物提供了一种通用的方法。这种方法允许以区域选择性和优异的总收率的方式,将易于获得的前体进行收敛组合。这种多取代异喹啉的强大合成途径不仅限于富电子部分,还可以快速获得具有生物活性的化合物的类似物。