Laboratory of Catalysis and Organic Synthesis, Ecole Polytechnique Fédérale de Lausanne, EPFL SB ISIC LCSO, BCH4306, 1015 Lausanne, Switzerland.
Beilstein J Org Chem. 2011;7:565-9. doi: 10.3762/bjoc.7.65. Epub 2011 May 4.
The Au(III)-catalyzed cyclization of 2-alkynylanilines was combined in a one-pot procedure with the Au(I)-catalyzed C3-selective direct alkynylation of indoles using the benziodoxolone reagent TIPS-EBX to give a mild, easy and straightforward entry to 2-substituted-3-alkynylindoles. The reaction can be applied to unprotected anilines, was tolerant to functional groups and easy to carry out (RT, and requires neither an inert atmosphere nor special solvents).
Au(III)催化的 2-炔基苯胺环化反应与 Au(I)催化的吲哚 C3-选择性直接炔基化反应在一锅法中结合使用苯并碘杂环戊酮试剂 TIPS-EBX，温和、简便地生成了 2-取代-3-炔基吲哚。该反应可以应用于未保护的苯胺，对官能团具有容忍性，易于进行（室温下进行，既不需要惰性气氛也不需要特殊溶剂）。
