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

摘要

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