The cyclization reaction of various 2-ethynylanilines, which were easily synthesized from 2-haloanilines by the palladium-catalyzed reaction with terminal alkynes, with tetrabutylammonium fluoride (TBAF) to yield 2-substituted indoles proceeded at refluxing or room temperature in THF in excellent yields without affecting the bromo, chloro, cyano, ethoxycarbonyl, and ethynyl groups.
A. Yasuhara, Y. Kanamori, M. Kaneko, A. Numata, Y. Kondo and T. Sakamoto, J. Chem. Soc., Perkin Trans. 1, 1999, 529 DOI: 10.1039/A808842J
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