State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Chinese Academy of Science, Lanzhou, People's Republic of China.
Org Lett. 2011 May 20;13(10):2598-601. doi: 10.1021/ol2007154. Epub 2011 Apr 14.
Highly substituted 3-iodoquinolines bearing different alkyl and aryl moieties can be synthesized in moderate to excellent yields (up to 99%) by 6-endo-dig iodocyclization of 2-tosylaminophenylprop-1-yn-3-ols with molecular iodine (I(2)) under mild conditions. The cyclization is highly regioselective and the resulting 3-iodoquinolines can be further functionalized by various coupling reactions.
通过温和条件下分子碘（I(2)）对 2-对甲苯磺酰氨基苯丙-1-炔-3-醇的 6-endo-内碘化环化反应，可以以中等至优异的收率（高达 99%）合成带有不同烷基和芳基部分的高取代 3-碘喹啉。环化反应具有高度的区域选择性，得到的 3-碘喹啉可以通过各种偶联反应进一步官能化。
