亲电试剂驱动的官能化喹啉的区域选择性合成。
Electrophile-driven regioselective synthesis of functionalized quinolines.
机构信息
State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Chinese Academy of Science, Lanzhou, People's Republic of China.
出版信息
Org Lett. 2011 May 20;13(10):2598-601. doi: 10.1021/ol2007154. Epub 2011 Apr 14.
PMID:21491872
Abstract
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.
摘要
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。
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