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 inhibitor pharmacophore.