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Synthesis 2007(12): 1841-1847
DOI: 10.1055/s-2007-983717
DOI: 10.1055/s-2007-983717
PAPER
© Georg Thieme Verlag Stuttgart · New YorkPdX2/CuX2-Catalyzed Annulation of 2-Ethynylbenzeneamines: Selective Synthesis of 2-Substituted 3-Halo-1H-indoles
Weitere Informationen
Received
6 March 2007
Publikationsdatum:
08. Juni 2007 (online)
Publikationsverlauf
Publikationsdatum:
08. Juni 2007 (online)
Abstract
A novel and effective protocol for the synthesis of 2-substituted 3-halo-1H-indoles by PdX2/CuX2-catalyzed annulations of 2-ethynylbenzeneamines has been developed. In the presence of PdX2 and CuX2, the annulation reactions of a variety of 2-ethynylbenzeneamines were conducted in moderate to good yields. It is noteworthy that only N-acetyl-protected 2-ethynylbenzeneamines can undergo the reaction successfully.
Key words
palladium(II) halide - copper(II) halide - annulation - 2-ethynylbenzeneamine - 2-substituted 3-halo-1H-indoles
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