One-pot synthesis of pyrimido[1,6-a]indol-1(2H)-one derivatives by a nucleophilic addition/Cu-catalyzed N-arylation/Pd-catalyzed C-H activation sequential process.
One-pot synthesis of pyrimido[1,6-a]indol-1(2H)-one derivatives by a nucleophilic addition/Cu-catalyzed N-arylation/Pd-catalyzed C-H activation sequential process.
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DOI：
10.1021/ol101041e
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发表时间：
2010-06
期刊：
影响因子：
5.2
通讯作者：
Zhijing Wang;Jianguo Yang;Fan Yang;W. Bao
中科院分区：
文献类型：
--
作者：
Zhijing Wang;Jianguo Yang;Fan Yang;W. Bao
描述了一种通过亲核加成/Cu催化N-芳基化/Pd催化C-H活化顺序过程一锅法合成嘧啶并[1,6-a]吲哚-1(2H)-酮衍生物的新颖且方便的方法。容易制备的邻偕二溴乙烯基异氰酸酯与N-烷基苯胺的反应以中等至良好的收率得到所需的吲哚衍生物。
A novel and convenient one-pot synthesis of pyrimido[1,6-a]indol-1(2H)-one derivatives through a nucleophilic addition/Cu-catalyzed N-arylation/Pd-catalyzed C-H activation sequential process is described. The reaction of easily prepared ortho-gem-dibromovinyl isocyanates with N-alkyl-anilines gave the desired indole derivatives in moderate to good yields.