Gao Jilong, Shao Yingying, Zhu Jiaoyan, Zhu Jiaqi, Mao Hui, Wang Xiaoxia, Lv Xin
Department of Chemistry, College of Chemistry and Life Sciences, Zhejiang Normal University , Jinhua 321004, People's Republic of China.
J Org Chem. 2014 Oct 3;79(19):9000-8. doi: 10.1021/jo501250u. Epub 2014 Sep 22.
A straightforward assembly of 1,2-disubstituted indoles has been developed through a Cu(II)-catalyzed domino coupling/cyclization process. Under aerobic conditions, a wide range of 1,2-disubstituted indole derivatives were efficiently and facilely synthesized from 2-alkynylanilines and boronic acids. 2-(2-Bromoaryl)-1-aryl-1H-indoles, which were selectively generated in one pot under the Cu catalysis, afforded the indolo[1,2-f]phenanthridines via Pd-catalyzed intramolecular direct C(sp(2))-H arylation. The one-pot tandem approaches to the polycyclic indole derivatives were also successfully achieved.
通过铜（II）催化的多米诺偶联/环化过程，已开发出一种直接合成1,2-二取代吲哚的方法。在有氧条件下，由2-炔基苯胺和硼酸高效且简便地合成了多种1,2-二取代吲哚衍生物。在铜催化下一锅法选择性生成的2-(2-溴芳基)-1-芳基-1H-吲哚，通过钯催化的分子内直接C(sp(2))-H芳基化反应得到吲哚并[1,2-f]菲啶。多环吲哚衍生物的一锅串联方法也成功实现。
