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Copper‐Catalyzed N ‐Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore
Author(s) -
Ackermann Lutz,
Barfüßer Sebastian,
Potukuchi Harish K.
Publication year - 2009
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.200900004
Subject(s) - pharmacophore , chemistry , domino , combinatorial chemistry , aryl , catalysis , cascade reaction , copper , stereochemistry , organic chemistry , alkyl
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.