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A mild route to indoles by cyclization of 2-(1-alkynyl)anilines is offered by the use of simple bases such as KOtBu, KH, or CsOtBu and N-methylpyrrolidinone (NMP) at room temperature. The reaction has a broad scope and allows the preparation of various functionalized indoles as well as new aza-or diazaindoles in excellent yields [see, for example, Eq. (1)].

Original publication

DOI

10.1002/1521-3773(20000717)39:14<2488::AID-ANIE2488>3.0.CO;2-E

Type

Journal article

Journal

Angewandte Chemie - International Edition

Publication Date

17/07/2000

Volume

39

Pages

2488 - 2490