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

Ackermann Lutz | Zendy; Barfüßer Sebastian | Zendy; Potukuchi Harish K. | Zendy

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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.

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