Copper‐Catalyzed N‐Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore

Copper‐Catalyzed N‐Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore

Inexpensive copper catalysts allow for efficient syntheses of N‐aryl‐, N‐acyl‐, or N‐H‐(aza)indoles starting from ortho‐alkynylbromoarenes. The broad scope of this domino N‐arylation/hydroamin(d)ation process is highlighted by the synthesis of highly functionalized indoles, as well as of a Chek1/KDR...

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Veröffentlicht in:Advanced synthesis & catalysis 2009-05, Vol.351 (7‐8), p.1064-1072
Hauptverfasser: Ackermann, Lutz, Barfüßer, Sebastian, Potukuchi, Harish K.
Format: Artikel
Sprache:eng
Schlagworte:
amination
arylation
catalysis
copper
hydroamination
indoles
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Zusammenfassung:Inexpensive copper catalysts allow for efficient syntheses of N‐aryl‐, N‐acyl‐, or N‐H‐(aza)indoles starting from ortho‐alkynylbromoarenes. The broad scope of this domino N‐arylation/hydroamin(d)ation process is highlighted by the synthesis of highly functionalized indoles, as well as of a Chek1/KDR inhibitor pharmacophore.
ISSN:1615-4150
1615-4169
DOI:10.1002/adsc.200900004