Mild and efficient cyclization reaction of 2-ethynylaniline derivatives to indoles in aqueous medium
Kou Hiroya*, Shin Itoh and Takao Sakamoto
*Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba-ku, Sendai 980-8578, Japan, Email: hiroyamail.tains.tohoku.ac.jp
K. Hiroya, S. Itoh, T. Sakamoto, Tetrahedron, 2005, 61, 10958-10964.
A copper(II)-catalyzed cyclization of 2-ethynylaniline derivatives to indoles can be carried out in a mixture of H2O and MeOH in the presence of 1-ethylpiperidine at room temperature. A catalyst recycling reaction system was established.
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Indoles, Copper(II) salt, 2-Ethynylaniline, Cyclization reaction